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.
申请公布号
EP2602258(B8)
申请公布日期
2016.09.28
申请号
EP20130157396
申请日期
2012.09.26
申请人
AICURIS GMBH & CO. KG
发明人
DR. SCHWAB, WILFRIED;BIRKMANN, ALEXANDER;VÖGTLI, KURT;HAAG, DIETER;LENDER, ANDREAS;GRUNENBERG, ALFONS;KEIL, BIRGIT;REHSE, JOACHIM