公开(公告)号：US20200299226A1

公开(公告)日：2020-09-24

申请号：US16894435

申请日：2020-06-05

申请人： Jiangxi Normal University

发明人： Junfeng ZHAO ,  Long HU ,  Silin XU ,  Zhenguang ZHAO

IPC分类号： C07C219/20 ,  C07C303/40 ,  C07D231/56 ,  C07D333/68 ,  C07C311/17 ,  C07C231/02 ,  C07C233/05 ,  C07D263/22 ,  C07D209/20 ,  C07D307/68 ,  C07C269/06 ,  C07C239/22 ,  C07D209/14 ,  C07D295/13 ,  C07K5/078 ,  C07D295/192 ,  C07D493/10 ,  C07K5/062 ,  C07K5/072 ,  C07D495/04 ,  C07C213/08

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.

公开(公告)号：US20190210957A1

公开(公告)日：2019-07-11

申请号：US16311747

申请日：2017-01-20

申请人： Jiangxi Normal University

发明人： Junfeng ZHAO ,  Long HU ,  Silin XU ,  Zhenguang ZHAO

IPC分类号： C07C219/20 ,  C07C213/08 ,  C07C311/17 ,  C07C303/40 ,  C07C231/02 ,  C07C233/05

CPC分类号： C07C219/20 ,  C07C213/08 ,  C07C231/02 ,  C07C233/05 ,  C07C303/40 ,  C07C311/17 ,  C07D209/20 ,  C07D231/56 ,  C07D263/22 ,  C07D307/68 ,  C07D333/68 ,  C07K5/06

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.