Rapid in-plate generation of benzimidazole libraries and amide formation using EEDQ
摘要:
A solution phase method for the preparation of etonitazene-related benzimidazoles and a general method for the preparation of amide derivatives in 96-well format have been developed for the generation of libraries of compounds in parallel. (C) 1997 Elsevier Science Ltd.
A new lipase, Ndbn, capable of efficiently catalyzing the amidation between esters and aromatic amines which are weak nucleophilic reagents was discovered. Furthermore, Ndbn exhibits the capability to catalyze the aminolysis of carboxylic acids without the need for preparing ester substrate or a strictly anhydrous reaction environment. Additionally, an unusual preference of Ndbn for aromatic amines