发明名称 |
N-[5-(Aminosulfony1)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acetamide mesylate monohydrate |
摘要 |
The present invention relates to an improved and shortened synthesis of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide and the mesylate monohydrate salt thereof by using boronic acid derivatives or borolane reagents while avoiding toxic organic tin compounds and to the mesylate monohydrate salt of N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)phenyl]acet-amide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions. |
申请公布号 |
US9340535(B2) |
申请公布日期 |
2016.05.17 |
申请号 |
US201214347287 |
申请日期 |
2012.09.26 |
申请人 |
AICURIS GMBH & CO. KG |
发明人 |
Schwab Wilfried;Birkmann Alexander;Vogtli Kurt;Haag Dieter;Lender Andreas;Grunenberg Alfons;Keil Birgit;Rehse Joachim |
分类号 |
C07D417/12 |
主分类号 |
C07D417/12 |
代理机构 |
Millen White Zelano and Branigan, PC |
代理人 |
Millen White Zelano and Branigan, PC ;Henter Csaba;Zelano Anthony |
主权项 |
1. A crystalline N-[5-(aminosulfonyl)-4-methyl-1,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)-phenyl]acetamide methanesulfonic acid monohydrate having a purity above 96 weight-%. |
地址 |
Wuppertal DE |