SCHWAB, WILFRIED W,BIRKMANN, ALEXANDER A,VOEGTLI, KURT K,HAAG, DIETER D,LENDER, ANDREAS A,GRUNENBERG, ALFONS A,KEIL, BIRGIT B,REHSE, JOACHIM J,.施瓦布,.比克曼,.弗格特利,.哈格,.倫德,.格瓦嫩博格,.凱爾,.雷澤
申请号：
HK16109165.2
公开号：
HK1220978A
申请日:
2014.09.02
申请国别(地区):
HK
年份:
2017
代理人:
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]acetamide 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.
