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The development of catalytic carbonylation reactions has increased considerably. Although many reviews/chapters/books on carbonylation reactions have been published, summaries on cheap metal-catalyzed catalytic carbonylation reactions of aryl halides and other chemical bonds with high dissociation energy C–Y (Y ​= ​O, N, H) are still very rare. Focusing on green and sustainable chemistry, this review summarizes and discusses the achievements on carbonylative transformations of aryl halides (C(sp2)–X) and strong bonds C–Y (Y ​= ​O, N, H) based on non-expensive metal catalysts (Co, Mn, Mo, Ni, Fe, Cu), photochemical and electrochemical systems developed in recent decades.

Abstract Four-membered carbocycles are among the most sought-after backbones which are commonly found in biologically active molecules. However, difficulties on their producing are existing due to its highly strained ring system. On the other hand, cyclobutanols can be straightforwardly prepared and can serves as precursors for synthesizing cyclobutane derivatives. Here we report an example of regioselective aminocarbonylation of cyclobutanols in which the cyclobutane core remained intact. The method exhibits good functional group compatibility, as well as high regio- and stereoselectivity, offering new pathways for synthesizing several pharmaceuticals. Furthermore, this strategy enables the rapid installation of cyclobutane as a conformational restricted skeleton, greatly facilitating direct access to valuable drug molecules that require conformational restriction.

Abstract Chiral amides are common and effective structural motifs found in many pharmaceuticals and biologically active molecules. Despite their importance, existing synthetic methods are predominantly employed for the synthesis of α-amides and β-amides. The synthesis of remote chiral amides, characterized by distal stereocenters, typically requires intricate synthetic steps conducted under demanding conditions. Here, we present a general procedure for the copper-catalyzed enantioselective synthesis of γ-chiral amides, employing a reductive relay hydroaminocarbonylation strategy with trisubstituted allylic benzoates and hydroxylamine electrophiles. This approach demonstrates a wide substrate scope with excellent enantioselectivity and regioselectivity, thus providing access to challenging enantioenriched γ-chiral amides.

Abstract Purpose This research evaluates the effect of balloon pulmonary angioplasty (BPA) on cardiac electrophysiological changes in patients with chronic thromboembolic pulmonary hypertension (CTEPH). Methods Involving a retrospective analysis of 39 CTEPH patients (average age 61 ± 11), who had at least two BPAs and paired ECGs pre- and post-surgery, we examined changes in ECG indicators of right ventricular hypertrophy and their correlation with hemodynamic results. Results BPA yielded marked improvements in cardiac function and hemodynamics. ECG parameters, specifically the Lewis criteria and Butler-Leggett score, correlated strongly with hemodynamics and were predictive of a mean pulmonary arterial pressure (mPAP) ≥ 35mmHg. Notably, QRS complex axis normalization was observed in 25 patients, with 14 fully normalizing (range − 30° to + 90°). The qR pattern in V1 vanished in 9 cases, and 75% of the patients in qR pattern in V1 group had QRS complex electrical axis completely returned to normal range. The qR V1 group had higher mPAP and pulmonary vascular resistance (PVR), and lower cardiac output and index compared to the non-qR V1 group, alongside a higher Butler-Leggett score. Conclusions BPA enhances cardiac function and hemodynamics in CTEPH patients, with certain ECG measures such as Lewis criteria and Butler-Leggett score reflecting the severity of hemodynamic impairment. The reversal of QRS axis deviation and the disappearance of the qR pattern in lead V1 may serve as valuable indicators for assessing post-BPA satisfaction in CTEPH patients.

Carbonylation processes have become widely recognized as a versatile, convenient, and low-cost method for the synthesis of high-value compounds. Given the great importance of heterocyclic compounds, the carbonylative approach has become increasingly important for their synthesis. In this mini-review, as a class of benzo-fused nitrogen-containing heterocyclic compounds, we summarized and discussed the recent achievements on the synthesis and functionalization of indole derivatives via carbonylative approaches.

Abstract γ-Amino acids and peptides analogues are common constituents of building blocks for numerous biologically active molecules, pharmaceuticals, and natural products. In particular, γ-amino acids are providing with better metabolic stability than α-amino acids. Herein we report a multicomponent carbonylation technology that combines readily available amides, alkenes, and the feedstock gas carbon monoxide to build architecturally complex and functionally diverse γ-amino acid derivatives in a single step by the implementation of radical relay catalysis. This transformation can also be used as a late-stage functionalization strategy to deliver complex, advanced γ-amino acid products for pharmaceutical and other areas.

Abstract Chronic wounds seriously affect the quality of life of the elderly, obese people, and diabetic patients. The excessive inflammatory response is a key driver of delayed chronic wound healing. Although lavender essential oil (EO [lav]) has been proven to have anti‐inflammatory and accelerate wound curative effects, the specific molecular mechanism involved is still ambiguous. The results showed that the wounds treated with lipopolysaccharide (LPS) not only had delayed healing, but also the expression levels of pro‐inflammatory cytokines, such as tumor necrosis factor‐α (TNF‐α), interleukin‐6 (IL‐6), interleukin‐1β (IL‐1β), and the inflammatory mediator protein, high‐mobility group box 1 protein (HMGB‐1), in the wound tissues were significantly increased. However, treatment of LPS‐induced chronic wounds with EO (lav) accelerated wound healing and decreased IL‐1β and HMGB‐1 expression levels. It was further found that LPS induced macrophage pyroptosis to produce IL‐1β. After treatment with EO (lav), the expression level of macrophage pyroptosis marker Gasdermin D (GSDMD) and pyroptosis‐related cytotoxic effects were significantly reduced. Immunofluorescence results also directly indicate that EO (lav) can protect macrophages from LPS‐induced pyroptosis. Moreover, EO (lav) can down‐regulate expression levels of IL‐1β, GSDMD, and nucleotide‐binding oligomerization domain‐like receptor protein 3 (NLRP3) in the caspase‐11‐related pyroptotic signaling pathway. This study demonstrates that EO (lav) can reduce proinflammatory factor production and ameliorate inflammatory response by inhibiting macrophage pyroptosis, which accelerates LPS‐induced chronic wound healing.

Background: Little is known about immediate responses of blood perfusion to the balloon pulmonary angioplasty (BPA) procedure. Objectives: To investigate the changes in pulmonary perfusion of balloon-dilated vessels and untreated vessels with before, immediately after a single BPA and at follow-up. Design: Retrospective single-center cohort study. Methods: Patients who had chronic thromboembolic pulmonary hypertension (CTEPH) and completed the pulmonary perfusion single photon emission computed tomography (SPECT) imaging before, immediately after BPA and at follow-up were included. We evaluated the perfusion defects of both-lung, BPA target (balloon dilated) and non-target (untreated) vessel segments according to Begic 3-point scale in each lung segment. Results: Forty patients (40 BPA procedures) were included and were given next BPA after 89 (62–125) days. The hemodynamic parameters including mPAP, PVR, and RAP were significantly improved after a single BPA. Visual scoring results of pulmonary perfusion imaging in 40 BPAs showed the perfusion defect scores of target vessels reduced from 5.6 ± 2.6 to 4.2 ± 2.2 ( p

Background & Aims: Immunotherapy is an option for the treatment of advanced biliary tract cancer (BTC), although it has a low response rate. In this post hoc analysis, we investigated the predictive value of an immuno-genomic-radiomics (IGR) analysis for patients with BTC treated with camrelizumab plus gemcitabine and oxaliplatin (GEMOX) therapy. Methods: Thirty-two patients with BTC treated with camrelizumab plus GEMOX were prospectively enrolled. The relationship between high-throughput computed tomography (CT) radiomics features with immuno-genomic expression was tested and scaled with a full correlation matrix analysis. Odds ratio (OR) of IGR expression for objective response to camrelizumab plus GEMOX was tested with logistic regression analysis. Association of IGR expression with progression-free survival (PFS) and overall survival (OS) was analysed with a Cox proportional hazard regression. Results: CT radiomics correlated with CD8+ T cells (r = –0.72–0.71, p = 0.004–0.047), tumour mutation burden (TMB) (r = 0.59, p = 0.039), and ARID1A mutation (r = –0.58–0.57, p = 0.020–0.034). There was no significant correlation between radiomics and programmed cell death protein ligand 1 expression (p >0.96). Among all IGR biomarkers, only four radiomics features were independent predictors of objective response (OR = 0.09–3.81; p = 0.011–0.044). Combining independent radiomics features into an objective response prediction model achieved an area under the curve of 0.869. In a Cox analysis, radiomics signature [hazard ratio (HR) = 6.90, p

Background: Histone deacetylase 3 (HDAC3) restores chromatin nucleosomes to a transcriptional repression state, thereby inhibiting gene expression. Studies have found that HDAC3 expression is upregulated in a variety of pathological states of the central nervous system and related to its neurotoxicity. However, the role of HDAC3 in surgical brain injury (SBI) has not been thoroughly explored. Objective: To observe the role of HDAC3 in SBI and the outcome of SBI after its suppression. Methods: Rat SBI model was used, and intraperitoneal injection of RGFP966 (HDAC3 specific inhibitor) was used to detect the changes of HDAC3 expression and neuronal apoptosis indexes in the surrounding cortex of SBI rats, and the cerebral edema and neurological outcome of rats were observed. Results: The expression of HDAC3 in the peripheral cortex of SBI rats was increased, and RGFP966 inhibited the upregulation of HDAC3 and saved the nerve cells around the damaged area. In addition, RGFP966 increased the expression of anti-oxidative stress proteins such as heme oxygenase-1 (HO-1) and superoxide dismutase 2 (SOD2). At the same time, the expression of apoptotic marker protein cleaved-caspase-3 (cle-caspase-3) was decreased, while the expression level of apoptotic protective marker protein B-cell lymphoma 2 (Bcl-2) was increased. In addition, this research demonstrated that in the RGFP966 rat SBI model, the expression level of antioxidant modifier nuclear factor-erythroid 2-related factor 2 (Nrf2) was increased. Conclusion: RGFP966 might activate HDAC3/Nrf2 signaling pathway by inhibiting HDAC3, regulated oxidative stress and nerve cell apoptosis induced by SBI in rat SBI model, reduced brain edema, and had a protective effect on nerve injury. It might be a potential target of SBI pathology.

Abstract Percutaneous endovascular biopsy (PEB) including forceps biopsy and catheter aspiration has been used to make a pretreatment diagnosis for pulmonary artery (PA) masses. This retrospective study aims to describe the procedure of PEB and compare the diagnostic yield of forceps biopsy and catheter aspiration for a definite diagnosis in patients with PA masses. All consecutive 22 patients (53 ± 14 years), 11 males and 11 females, who underwent PEB for pathologic confirmation between November 2018 and November 2022 were enrolled. All 22 patients performed computed tomography pulmonary angiography or positron emission tomography‐computed tomography to confirm the filling defects suspicious for PA malignancy before intervention. And then, all patients underwent PEB successfully without acute or fatal complications, including both forceps biopsy and catheter aspiration in 15 cases, only forceps biopsy in 5 cases, and only catheter aspiration in 2 cases. Histopathological analysis provided a definite diagnosis in all PEBs with a clinical success of 91.0% (20/22). Among them, in 15 patients who underwent both forceps biopsy and aspiration biopsy, the technical success using forceps biopsy was 93.3% (14/15), and aspiration biopsy was 6.7% (1/15), and there was a significant difference in diagnostic accuracy when comparing two techniques. Twenty‐one out of 22 PA masses (95.5%) were malignant, of which, the most frequent malignant lesion observed was PA sarcoma (66.7%, 14/21). Benign lesion included one thrombus (4.5%, 1/22). In conclusion, PEB is an effective and safe diagnostic method for differentiating benign and malignant PA masses and could be peformed when PA masses appeared clinically malignant.

A convenient approach for the construction of pharmaceutically valuable 3-trifluoromethyl-1,2,4-triazoles has been developed, which employs the readily available trifluoroacetimidoyl chlorides, hydrazine hydrate and benzene-1,3,5-triyl triformate (TFBen) as starting materials. The multi-component reaction features broad substrate scope, high efficiency, and scalability, providing a facile and straightforward route to the biologically important 3-trifluoromethyl-1,2,4-triazole scaffolds in moderate to good yields. Considering its broad-spectrum pharmaceutical activity, the method offers the opportunity for the further study towards the toxicity risk assessment and structure-activity relationship of the pharmaceuticals containing trifluoromethyl-1,2,4-triazole cores.

Succinates play a vital role in industry, pharmaceutics, beverage, and cosmetics. A regio- and stereoselective alkoxycarbonylation of unsymmetrical internal alkynes with alcohols or phenols toward α, β-unsaturated succinates enabled by palladium catalysis has been accomplished under mild conditions. A series of α, β-unsaturated succinates with a broad range of functional groups were obtained in exclusive (E)-stereoselectivity and good yields. Furthermore, (Z)-stereoselectivity α, β-unsaturated can be obtained by a simple photocatalytic isomerization reaction.

Abstract Background Emerging evidence suggests that epithelial mesenchymal transition (EMT) and epigenetic mechanisms promote metastasis. Histone deacetylases (HDACs) and noncoding RNAs (ncRNAs) are important epigenetic regulators. Here, we elucidated a novel role of histone deacetylase 2 (HDAC2) in regulating EMT and CRC metastasis via ncRNA. Methods The expression of HDACs in CRC was analyzed using the public databases and matched primary and metastatic tissues, and CRC cells with different metastatic potentials (DLD1, HCT116, SW480 and SW620). Microarray analysis was used to identify differential genes in parental and HDAC2 knockout CRC cells. EMT and histone modifications were determined using western blot and immunofluorescence. Migration ability was assessed by transwell assay, and metastasis was assessed in vivo using a tail vain injection. Gene expression and regulation was assessed by RT-PCR, chromatin immunoprecipitation and reporter assays. Protein interaction was assessed by immunoprecipitation. Specific siRNAs targeting H19, SP1 and MMP14 were used to validate their role in HDAC2 loss induced EMT and metastasis. Results Reduced HDAC2 expression was associated with poor prognosis in CRC patients and found in CRC metastasis. HDAC2 deletion or knockdown induced EMT and metastasis by upregulating the long noncoding RNA H19 (LncRNA H19). HDAC2 inhibited LncRNA H19 expression by histone H3K27 deacetylation in its promoter via binding with SP1. LncRNA H19 functioned as a miR-22-3P sponge to increase the expression of MMP14. HDAC2 loss strongly promoted CRC lung metastasis, which was suppressed LncRNA H19 knockdown. Conclusion Our study supports HDAC2 as a CRC metastasis suppressor through the inhibition of EMT and the expression of H19 and MMP14.

Folates, provided by food, are commonly used antidepressant synergists in late-onset depression (LOD). However, increased intake of folic acid in the elderly population might lead to the accumulation of unmetabolized folic acid in the systemic circulation, leading to enhanced deterioration of the central nervous system function. In addition, folates cannot access the brain directly because of the blood–brain barrier. Choroid plexus (CP) 5-methyltetrahydrofolate (5-MTHF) brain transport plays a critical role in regulating the cerebrospinal fluid (CSF) 5-MTHF content. Luteolin is a natural flavonoid that has antidepressant effects and is involved in the anti-folate resistance pathway. It remains unclear whether the antidepressant effects of luteolin are associated with the CP 5-MTHF brain transport. In this study, 20–21-month-old Wistar rats were exposed to the chronic unpredictable mild stress (CUMS) protocol for 6 consecutive weeks to explore the long-term effects of luteolin on behavior, 5-MTHF levels, hippocampal neurogenesis, and folate brain transport of the CP. In vitro primary hippocampal neural stem cells (NSCs) cultured in media containing 10% CSF from each group of rats and choroid plexus epithelial cells (CPECs) cultured in media containing 20 μM luteolin were treated with 100 μM corticosterone and 40 mg/ml D-galactose. We found that aged rats exposed to CUMS showed a significantly reduced sucrose preference, decreased locomotion activity in the open field test and accuracy of the Morris water maze test, increased immobility time in the forced swimming test, accelerated dysfunctional neurogenesis and neuronal loss in the dentate gyrus of LOD rats, as well as decreased CSF and hippocampus 5-MTHF levels, and zona occludens protein 1 (ZO-1), proton-coupled folate transporter (PCFT), and reduced folate carrier (RFC) protein levels. In vitro assays showed media containing 10% aged CSF or LOD+ Luteolin-CSF significantly increased the viability of CORT + D-gal-injured NSCs and alleviated dysfunctional neurogenesis and neuronal loss compared with the CORT + D-gal medium. However, media containing 10% LOD-CSF had no such effect. In the meantime, induction of CORT + D-gal significantly decreased the ZO-1, PCFT, RFC, and folate receptor alpha (FR-α) protein levels and transepithelial electrical resistance in rat CPECs. As expected, luteolin treatment was effective in improving these abnormal changes. These findings suggested that luteolin could ameliorate CUMS-induced LOD-like behaviors by enhancing the folate brain transport.

Palladium nanoparticles supported on low-melting polyester (Pd/LMPET) fabric were prepared through a microwave irradiation assisted method. In this way, in situ growth of Pd nanoparticles onto an easy to handle material was initiated and proceeded. The results of the characterization revealed that the palladium nanoparticles were well-dispersed on the surfaces of the polyester fibers. The Pd/LMPET fabrics were then employed in the Suzuki-Miyaura coupling. They exhibited excellent catalytic activity in ethanol/water under air atmosphere at 50 °C. Importantly, the Pd/LMPET fabrics could be separated from reaction mixture conveniently and they can still maintain good activity after 8 cycles without Pd leaching.

The isoquinolinamine FX-9 is a novel potential chemotherapeutic agent showing antiproliferative effects against hematologic and prostate cancer cell lines such as B- and T-acute lymphoblastic leukemia and prostate cancer (PC) of different species. Interestingly, FX-9 shows no hemolytic activity and low toxicity in benign adherent cells. The detailed FX-9 molecular mode of action is currently not fully understood. But application on neoplastic cells induces pro-apoptotic and antimitotic effects. Canine prostate cancer (cPC) represents a unique spontaneous occurring animal model for human androgen-independent PC. Human androgen-independent PC as well as cPC are currently not satisfactorily treatable with chemotherapeutic protocols. Accordingly, the evaluation of novel agent combinations bears significant potential for identifying novel treatment strategies. In this study, we combined FX-9 with the currently approved therapeutic agents doxorubicin, carboplatin, the demethylating substance azacitidine as well as further potentially antitumorigenic agents such as dichloroacetic acid (DCA) in order to evaluate the respective synergistic potential. The combinations with 1-5 μM FX-9 were evaluated regarding the effect after 72 hours on cell viability, cell count and apoptotic/necrotic cells in two human prostate cancer cell lines (LNCaP, PC-3) and a canine prostate cancer cell line (Adcarc1258) representing androgen-dependent and -independent PC/cPC forms. FX-9 in combination with azacitidine decreases cell viability and increases cell death with positive Bliss values. Furthermore, this decreases the cell count with neutral Bliss values on PC-3. Carboplatin in combination with FX-9 reduces cell viability with a neutral Bliss value and increases cell death on LNCaP with calculated positive Bliss values. DCA or doxorubicin in combination with FX-9 do not show synergistic or additive effects on the cell viability. Based on these results, azacitidine or carboplatin in combination with FX-9 offers synergistic/additive efficacy against prostate adenocarcinoma cell lines in vitro. The beneficial effects of both combinations are worth further investigation.

Herein, we developed a rhodium-catalyzed reduction of CO with bis(pinacolato)diboron (B2pin2) under atmospheric pressure of CO with silane as the hydride source, gem-diborylmethane [H2C(Bpin)2] as a versatile and fundamental C1 compound can be formed. Notably, this is the first example on transition metal-catalyzed borylation of CO.

A nickel-catalyzed carbonylative synthesis of dihydrobenzofurans has been developed. With Mo(CO)6 as the CO source and manganese metal as the reductant, alkyl halides were reacted with aryl iodides to give the desired products in moderate to good yields.

Summary: Functionalized alkyl iodides are important compounds in organic chemistry and biology. In this communication, we developed an interesting nickel-catalyzed carbonylative synthesis of functionalized alkyl iodides from aryl iodides and ethers. With Mo(CO)6 as the solid CO source, both cyclic and acyclic ethers were activated, which is also a challenging topic in organic synthesis. Functionalized alkyl iodides were prepared in moderate to excellent yields with outstanding functional group tolerance. Besides the high value of the obtained products, all the atoms from the starting materials were incorporated in the final products and the reaction had high atom efficiency as well. : Chemistry; Catalysis; Organic Synthesis Subject Areas: Chemistry, Catalysis, Organic Synthesis

Summary: The synthetic utilities of acylgermanes are surprisingly rarely explored compared with their analogues. In this communication, the survey of aroyltrimethylgermane as potent synthetic origins has been studied. A variety of novel chemical transformations have been realized, including using the acylgermane group as a directing group in Rh-catalyzed aromatic C-H alkenylation reaction and Ir-catalyzed aromatic C-H amidation reactions. Additionally, a general approach for acylgermanes preparation has been established as well. The catalytic system proceeds effectively in the presence of Pd(OAc)2/BINOL-based monophosphite (L11) and allows for the straightforward access to a wide range of functionalized acylgermanes in high yields. : Catalysis; Organic Synthesis; Organic Reaction; Chemical Synthesis Subject Areas: Catalysis, Organic Synthesis, Organic Reaction, Chemical Synthesis

This paper puts forward the concept of incentive utility, which converts the value of each attribute in multi-attribute decision-making into a unified index for measurement, thus simplifying multi-attribute decision-making. In this paper, a comprehensive evaluation model based on the TOPSIS of incentive utility is established. Through the establishment of incentive index, the utility of incentive and the calculation of ideal point of utility, the disadvantage of "ideal point is not ideal" in the TOPSIS is overcome. It can better synthesize the sub-attribute value and realize the subjective multi-attribute decision-making. The example shows that the model can apply subjective factors to decision-making scientifically, and the result is more reasonable and effective.

Background: Liver transplantation has become the treatment of choice for patients with end-stage acute or chronic hepatic disease. Bile duct complications are common events after liver transplantation. The aim of this study was to evaluate the blood supply of the human bile duct and identify the underlying mechanisms of bile duct complications after liver transplantation. Methods: The duct supply branches from gastroduodenal artery and blood supply of extrahepatic bile duct system were re-evaluated through selective hepatic angiography from 600 patients. In addition, 33 cadavers were injected with latex casting material into the common hepatic artery, then the extrahepatic bile duct and the branches from the common hepatic artery were carefully dissected to visualize the gastroduodenal artery and its branching to the extrahepatic bile duct. Results: The bile duct artery arose from the branch of the gastroduodenal artery in 8.1% (49/600). Of these 49 individuals, the bile duct artery was supplied by the gastroduodenal artery (61.22%, 30/49), the proper hepatic artery (14.29%, 7/49), or both the gastroduodenal artery and the proper hepatic artery (24.49%, 12/49). In our study of 33 cadavers, the percentage that the bile duct artery arose from the gastroduodenal artery was 27.27%. The blood supply to the bile extrahepatic bile ducts was divided into different segments and formed longitudinal and arterial network anastomosed on the walls of the duct. Conclusions: There is a close relationship between the duct supply branches from gastroduodenal artery and the blood supplying patterns of the extrahepatic bile duct system. In liver transplant surgery, the initial part of the gastroduodenal artery is preferred to be preserved in the donor liver. It is of great significance to improve the success rate of operation and reduce complications.

A simple transition metal-free procedure using formal dehyde for the N,N-dimethylation and N-methylation of primary and secondary anilines is reported. The reaction showed limitations on sterically hindered and electron-withdrawing anilines, but is successful on amines with electron-donating substituents. Formaldehyde acts as both the reducing agent and the carbon source in the reaction.

Existing robust Capon beamformers achieve robustness against steering vector errors at a high cost in terms of computational complexity. Computationally efficient robust Capon beamforming approach based on the reduced-rank technique is proposed in this paper. The proposed method projects the received data snapshots onto a lower dimensional subspace consisting of the matched filters of the multistage Wiener filter (MSWF). The subsequent adaptive beamforming will then be performed within this subspace. The combination of the benefit of the robust adaptive beamforming and the reduced-rank technique improves the performance on combating steering vector errors and lowering the computational complexity.

Existing subspace-based direction finding methods for multiple-input multiple-output (MIMO) radar assume perfect knowledge about the dimension of the signal or noise subspace, which is hard to be established without prior knowledge of the signal environment. In this paper, an efficient method for joint DOA and DOD estimation in bistatic MIMO radar without estimating the number of targets is presented. The proposed method computes an estimate of the noise subspace using the power of R (POR) technique. Then the two-dimensional (2D) direction finding problem is decoupled into two successive one-dimensional (1D) angle estimation problems by employing the rank reduction (RARE) estimator.

Herein we report an interesting copper-catalyzed transformation of BCBs with diazo compounds. This reaction leads to the synthesis of substituted skipped penta-1,4-dienes in good to excellent yields with only one diastomer obtained, and the reaction can also be performed on a gram scale. The transformation is compatible with many different functional groups attached to the BCBs and the diazo compounds. [ABSTRACT FROM AUTHOR]

Background: Symptomatic intracranial in-stent restenosis (sISR) poses a major challenge in the management of cerebrovascular diseases, often requiring effective and safe treatment options. Objectives: This study aims to evaluate the efficacy and safety of paclitaxelcoated balloon (PCB) angioplasty for treating sISR. Methods: We conducted a retrospective analysis of five patients aged 49-74 years, who were treated with PCB angioplasty between January 2017 and June 2022. Treatment procedures included pre-operative digital subtraction angiography, antiplatelet therapy, and the use of the SeQuent Please balloon. Patients received aspirin and clopidogrel prior to and after the procedure. Results: The procedure achieved a 100% success rate. The degree of ISR was significantly reduced from an average pre-operative rate of 72±18.9% to a postoperative rate of 34±8.22%. Long-term follow-up showed that the majority of patients did not experience restenosis, confirming the long-term effectiveness of the treatment. Conclusions: PCB angioplasty demonstrates significant potential as an effective and safe treatment option for patients with sISR, especially those considered to be at high risk. This study supports further investigation into PCB angioplasty as a standard treatment for sISR. [ABSTRACT FROM AUTHOR]