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-12258318-B2 优先权日:2019-06-17 标题 :Synthesis method for 1-methyl-1H-indazole-6-carboxylic acid 发明人:YANG JUN; Xue Duoqing; WU YONG; CHEN LIHUANG; ZHAI LIANHUA 权利人:ACCELA CHEMBIO CO LTD 摘要:The present application provides a synthesis method for 1-methyl-1H-indazole-6-carboxylic acid. The synthesis method comprises: using 2-fluoro-4-bromobenzaldehyde and methylhydrazine as raw materials to obtain 6-bromo-1-methylindazole by means of an annulation reaction, and then performing a methyl formate reaction and a hydrolysis reaction, so as to obtain the 1-methyl-1H-indazole-6-carboxylic acid. The synthesis method provided in the present application can directly synthesize a 1-position methyl substituted indazole without isomers, thereby avoiding the problem that impurities are difficult to be removed in subsequent separation, thus improving the purity of a product. The yield of the annulation reaction can reach 85%.
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:EP-3515880-B1 优先权日:2017-03-17 标题:Methods and compositions for synthesis of encoded libraries 发明人:LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN 权利人:HITGEN INC
专利号:US-2020149034-A1 优先权日:2017-03-17 标题:Methods and Compositions for Synthesis of Encoded Libraries