Center for Drug DiscoVery & Design and State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Shanghai Institutes for Biological Sciences, Chinese Academy of Sciences, 294 Taiyuan Road, Shanghai 200031, P. R. China, Chemical Process & Biotechnology Department, Singapore Polytechnic, 500 DoVer Road, Singapore 139651, Department of Structural Biology, Weizmann Institute of S...

A method is described which provides for the direct asymmetric catalytic synthesis of trisubstituted aziridines from imines and diazo compounds. While unactivated imines were not reactive to α-diazo carbonyl compounds in which the diazo carbon was disubstituted, N-Boc imines react with both α-diazo esters and α-diazo-N-acyloxazolidinones to give trisubstituted aziridines with excellent diastere...

N-aryl imidazoles play an important role as structural and functional units in many natural products and biologically active compounds. Herein, we report a photocatalytic route for the C-N cross-coupling reactions over a Cu/graphene catalyst, which can effectively catalyze N-arylation of imidazole and phenylboronic acid, and achieve a turnover frequency of 25.4 h(-1) at 25°C and the irradiation...

A variety of heteroaromatic compounds, such as substituted pyridines, pyrazoles, indoles, 2-substituted imidazoles, 2-substituted imidazoles, 2-arylbenzazoles and pyrimidin-2(1H)-ones are synthesized by oxidative aromatization using the activated carbon and molecular oxygen system. Mechanistic study focused on the role of activated carbon in the synthesis of 2-arylbenzazoles is also discussed. ...

An enantioselective Friedel-Crafts alkylation with alpha,beta-unsaturated 2-acyl imidazoles and electron-rich aromatic nucleophiles catalyzed by bis(oxazolinyl)pyridine-scandium(III) triflate complexes has been accomplished. These alpha,beta-unsaturated 2-acyl imidazoles are effective electrophiles for the Friedel-Crafts reaction. The resulting adduct 2-acyl imidazole is easily converted to ami...

An efficient approach to the synthesis of 1,2,3-trisubstituted indolizines is described via one-pot reactions of pyridine and dialkyl acetylendicarboxylate in the presence of ethyl 2-chloroacetoacetate in MeOH at room temperature. The corresponding 1, 2, 3-trisubstituted indolizines may be useful building blocks for the construction of complex indolizine derivatives.

The microwave assisted and solvent free synthesis of title compounds is described in this protocol. Ten new aryl imidazoles, which are incorporated with the chemotherapeutic pharmacophores, have been synthesized by adopting one pot multicomponent reaction. First, primary aromatic or heteryl amine has been condensed with aryl or heteryl aldehydes to afford corresponding Schiff base. The Schiff b...