发明名称 Process for preparing N-H or N-alkyl 2-propynamide
摘要 Disclosed is a method for the synthesis of N—H or N-alkyl 2-propynamides useful as intermediate in the manufacture of pharmaceutically active ingredients.
申请公布号 US8895780(B2) 申请公布日期 2014.11.25
申请号 US201314013098 申请日期 2013.08.29
申请人 Boehringer Ingelheim International GmbH 发明人 Deng Da;Zheng Juncheng
分类号 C07C231/02 主分类号 C07C231/02
代理机构 代理人 Morris Michael P.;Devlin Mary-Ellen M.
主权项 1. A method of preparing N—H or N-alkyl 2-propynamides of formula (I) wherein R1 is hydrogen or C1-4-alkyl, said process comprising reacting a propiolic acid ester of formula (II) wherein R2 is C1-2-alkyl, with an amine of the formula (III) wherein R1 is defined as in formula (I), in water, and at a reaction temperature from of about −10° C. to about 10° C. to form a compound of formula (I).
地址 Ingelheim am Rhein DE