发明名称 PROCESS FOR PREPARATION OF RUFINAMIDE
摘要 The present invention relates to a novel process for preparation of rufinamide (I) comprising: reacting 2,6-difluorobenzyl azide (II) and propiolic acid (III) in a mixture of alcohol and water to produce 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid (IV), esterifying the acid (IV) to ester (V) and treating ester (V) with ammonia. The invention further relates to process for purification of 1-(2,6-difluorobenzyl)-1H-1,2,3-triazole-4-carboxylic acid (IV), by crystallization from a mixture of alcohol and water. The present invention also provides process for purification of rufinamide (I) by crystallization from mixture of polar aprotic solvent with water or alcohol.
申请公布号 US2014357871(A1) 申请公布日期 2014.12.04
申请号 US201314369811 申请日期 2013.01.09
申请人 LUPIN LIMITED 发明人 Siyan Rajinder Singh;Aher Yogesh Subhas;Bhise Nandu Baban;Singh Girij Pal;Gohel Sunilkumar Vinubhai
分类号 C07D249/04 主分类号 C07D249/04
代理机构 代理人
主权项
地址 Mumbai, Maharashtra IN