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Using microwave technology, rapid ω-methoxylation of aryl alkynes is possible. [Copyright &y& Elsevier]

The use of catalytic fast pyrolysis (CFP) of biomass to produce high-quality bio-oils as potential substitutes for conventional fuels plays an essential role in the decarbonization of the world. In this study, continuous CFP tests of sawdust using three commercial-ready catalysts were performed. The overall objective is to screen appropriate catalysts and catalyst loading amounts for further commercialization and upgrading by evaluating the quality of the organic fraction bio-oils and clarifying the relationship between the hydrogen-to-carbon atomic effective (H/C eff) ratio and bio-oil yield. The results displayed that, owing to a cracking effect of the catalyst, all catalytic cases had higher H/C eff ratios and larger relative area percentages of hydrocarbons determined by NMR. Thermogravimetric analysis reveals that, compared to non-catalytic bio-oils, catalytic bio-oils showed more distillates in the diesel range. Increasing the catalyst-loading amount also showed the same effect. Overall, all bio-oil products from catalytic cases had H/C eff ratios higher than 0.6, indicating the production of promising oil for hydrodeoxygenation. By analyzing and fitting the data from this work and comparing with the literature, it could be concluded that its yield would decrease as the bio-oil product quality increases (the H/C eff ratios increase). [Display omitted] • Continuous CFP tests were conducted, providing insight for scaling up. • Three different commercial-ready catalysts with two WHSV values were studied. • All catalysts-induced oil products with H/C eff higher than 0.6. • SA catalyst induced the most attractive oil production at WHSV of 0.5. • A negative correlation between H/C eff ratio and bio-oil yield was verified. [ABSTRACT FROM AUTHOR]

Abstract: AZD9272 and AZD6538 are two novel mGluR5 negative allosteric modulators selected for further clinical development. An initial high-throughput screening revealed leads with promising profiles, which were further optimized by minor, yet indispensable, structural modifications to bring forth these drug candidates. Advantageously, both compounds may be synthesized in as little as one step. Both are highly potent and selective for the human as well as the rat mGluR5 where they interact at the same binding site than MPEP. They are orally available, allow for long interval administration due to a high metabolic stability and long half-lives in rats and permeate the blood brain barrier to a high extent. AZD9272 has progressed into phase I clinical studies. [Copyright &y& Elsevier]

Abstract: A series of potent antagonists of the ion channel transient receptor potential A1 (TRPA1) was developed by modifying lead structure 16 that was discovered by high-throughput screening. Based on lead compound 16, a SAR was established, showing a narrow region at the nitro-aromatic R1 moiety and at the warhead, while the R2 side had a much wider scope including ureas and carbamates. Compound 16 inhibits Ca2+-activated TRPA1 currents reversibly in whole cell patch clamp experiments, indicating that under in vivo conditions, it does not react covalently, despite its potentially electrophilic ketone. [Copyright &y& Elsevier]

Abstract: Structure–activity relationship investigations of the thiopyrimidine (1), an HTS hit with micromolar activity as a metabotropic glutamate receptor 5 (mGluR5) antagonist, led to compounds with sub-micromolar activity. [Copyright &y& Elsevier]