摘要 |
<p>The invention describes an improved process for the manufacture of a Flecainide intermediate viz N-(pyridin-2-ylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide (II). It consists of reacting 2,5-bis(2,2,2-trifluoroethoxy)benzoic acid with an acid chloride in a solvent mixture in presence of a base at−10 to−50° C. The resulting mixed anhydride is then condensed with 2-aminomethylpyridine at−10 to−40° C. and the resulting product after aqueous workup is purified by crystallization. This affords the intermediate II in vastly improved yields and quality. The intermediate II on catalytic hydrogenation affords N-(2-piperidinylmethyl)-2,5-bis(2,2,2-trifluoroethoxy)benzamide (Flecainide), isolated as its acetate.</p> |
申请人 |
GLADE ORGANICS PRIVATE LIMITED |
发明人 |
CHAWLA, HARMANDER PAL SINGH;CHOWDHARY, ANIL SHANKAR;LIMBAD, PIYUSH BHIKHUBHAI;JHA, RAJESH JAGANNATHBHAI;JOSHI, VIPUL NARBHESHANKAR |