Metodo para sintetizar n-[5-(aminosulfonil)-4-metil-1,3-tiazol-2-il]-n-metil-2-[4-(2-piridinil) fenil)]acetamida y mesilato monohidrato cristalino del mismo; composicion farmaceutica que lo contiene; combinacion farmaceutica; uso en el tratamiento y/o profilaxis de una infeccion por virus herpes simplex.

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.