SCHWAB, WILFRIED,BIRKMANN, ALEXANDER,VOGTLI, KURT,HAAG, DIETER,LENDER, ANDREAS,GRUNENBERG, ALFONS,KEIL, BIRGIT,REHSE, JOACHIM
申请号:
PH12015502801
公开号:
PH12015502801A1
申请日:
2015.12.16
申请国别(地区):
PH
年份:
2016
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]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.