Search

With the development of ortho C-H functionalization in Pd/NBE chemistry, the catalytic systems used are becoming increasingly complex. The increasingly complex catalytic systems may have created technical barri-ers for researchers in other fields to apply Pd/NBE chemical methods. This report describes the use of a simple Pd/NBE catalytic system to achieve ortho C-H oxylation and phosphonylation and other functionalization of iodobenzene through templated conversion reactions. The key point of this method is to explore the previous-ly unknown step of introducing dimethylamine in the ortho position of iodobenzene through C-H amination. Aryl dimethylamine is quickly converted to methyl quaternary ammonium salt precipitation, and methyl qua-ternary ammonium salt effectively avoids Hofmann elimination in the subsequent functionalization.

An efficient palladium-catalyzed Hiyama reaction between various pyrimidin-2-yl tosylates with organosilanes has been developed. The use of CuCl with TBAF as additive is essential for promotion of the construction of the carbon–carbon bond. This procedure shows wide functional group tolerance for electrophilic pyrimidin-2-yl tosylates and has been extended to aromatic amino-substituted pyrimidin-2-yl tosylates, affording the desired C2-aryl and alkenyl pyrimidine derivatives in good to excellent yields.

Glycerol is a new green organic solvent. It not only acts as a phase transfer catalyst but also as a recyclable solvent by significantly enhancing the intramolecular cyclization. A series of 4-aryl-7,7 -dimethyl-5-oxo-3,4,5,6,7,8-hexahydrocoumarin derivatives were synthesized by one-pot multicomponent reaction of Meldrum’s acid with benzaldehyde, and cyclohexanedione in glycerol. Compared to classic methods, this method has the advantages of milder reaction conditions, good yields, easy processing and environmental benignity.

A AgSCF

New 2-(1,2,3-triazol-1-yl)pyrimidines were synthesized in good yields by the three-component reaction of pyrimidin-2-yl sulfonates, sodium azide and active methylene ketones in the presence of K2CO3 at room temperature. This procedure eliminates the need to handle organic azides in the synthesis of analogous compounds.

A rapid and efficient method for the preparation of new pyrido[2,3-d]pyrimidinone derivatives by the condensation of 2-amino-4-aryl-6-arylnicotinamides with carbon disulfide or cycloalkanones under focused microwave irradiation is described.

Novel thiazolo[2,3-b]quinazolines were prepared by the cyclization reaction between octahydroquinazoline-2-thiones with α-bromoketones, which provides a readily accessible multifunctionalized quinazoline template for diversity-oriented synthesis.

The aza-Michael addition reaction of 4-aryl-7,7-dimethyl-1,2,3,4,5,6,7,8-octahydroquinazoline-2-one/thione-5-ones to α,β-ethylenic compounds in the presence of KF/Al2O3 furnishes N3-substituted quinazolinone derivatives. Those groups (NO2, MeO) with larger steric hindrance at the o-position of the phenyl ring of quinazolinone have an apparent affect on the chemical selectivity thus giving the N1-subsituted products.

Using rare earth nitrates, tryptophan (L), and sodium citrate (NaL′), three new rare earth ternary complexes (Nd-L-L′· 4H2O, Eu-L-L′ · 4H2O, and La-L-L′ · 4H2O) were prepared. The complexes were characterized by IR, molar conductivity, TG-DTA (thermo gravimetric-differential thermal analysis), 1H NMR, and elemental analyses. TG and elemental analyses of the prepared complexes showed good agreement with their stoichiometry. Compared with two individual ligands, IR spectra of synthesized complexes showed dramatic shift and intensity changes; 1H NMR also showed a slight downfield shift. All analytical results of complexes proved constant composition of M-L-L′ · 4H2O (M = rare earth metal, namely Nd, Eu, or La). Animal tests were also performed to study the anti-coagulation time of these complexes considering also the different concentration of complex Nd-L-L′ · 4H2O. PC-12 pheochromocytoma cells were used to study cell adhesion. Compared with ions of rare earth compounds, rare earth ternary complexes have lower cell toxicity, better cell adhesion, and better anticoagulant action.