N-[5-(AMINOSULFONYL)-4-METHYL-1,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2-PYRIDINYL)PHENYL]ACETAMIDE MESYLATE MONOHYDRATE

摘要

31 N-[5-(AMINOSULFONYL)-4-METHYL-l,3-THIAZOL-2-YL]-N-METHYL-2-[4-(2- PYRIDINYL)PHENYL]ACETAMIDE MESYLATE The present invention relates to an improved and shortened synthesis of N-[5- (aminosulfonyl)-4-methyl-l,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-l,3-thiazol-2-yl]-N-methyl-2-[4-(2-pyridinyl)- phenyl] acetamide which has demonstrated increased long term stability and release kinetics from pharmaceutical compositions. [No Figure]