专利号:US-11414375-B2 优先权日:2016-07-29 标题:Mild and efficient preparation method for α-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide 发明人:ZHAO JUNFENG; HU LONG; XU SILIN; ZHAO ZHENGUANG 权利人:UNIV JIANGXI NORMAL 摘要:Disclosed are a mild and efficient preparation method for an α-acyloxyenamide compound and a use thereof in the synthesis of an amide and a polypeptide. The α-acyloxyenamide compound is obtained by an addition reaction of a ynamide and a carboxylic acid in dichloromethane under conditions where the temperature is 0° C. to 50° C.; the produced α-acyloxyenamide compound can react with an amine compound to produce an amide or a polypeptide; the two reactions can be carried out step by step, and can also be carried out in one pot. According to the invention, the reaction conditions are mild and no metal catalyst is required; when the carboxylic acid, which has chirality on an alpha site of carboxyl, forms an amide bond or a peptide bond, no racemization occurs; and the operation is simple and the application range is wide.
专利号:US-8188282-B2 优先权日:2006-07-15 标 题:Regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; HALLAND NIS; RKYEK OMAR; URMANN MATTHIAS; SANOFI AVENTIS 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct palladium catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides useful for the production of pharmaceuticals, diagnostic agents, liquid crystals, polymers, herbicides, fungicidals, nematicidals, parasiticides, insecticides, acaricides and arthropodicides.
专利号:US-2020299226-A1 优先权日:2016-07-29 标题:Mild and efficient preparation method for a-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide
专利号:US-10836707-B2 优先权日:2016-07-29 标 题:Mild and efficient preparation method for α-acyloxyenamide compounds and use thereof in synthesis of amide and polypeptide
专利号:AU-2007276514-A1 优先权日:2006-07-15 标题:A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
专利号:CA-2657717-A1 优先权日:2006-07-15 标 题 :A regioselective palladium catalyzed synthesis of benzimidazoles and azabenzimidazoles
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