Aminolysis process for preparation of Lafutidine or pharmaceutically acceptable salts.

Abstract

This invention provides a process for the prepn. of Lafutidine or pharmaceutically acceptable salts, which comprises aminolysis of 2-[(2Z)-4-[[4-(1-piperidinylmethyl)-2-pyridinyl]oxy]-2-butenyl]-1H-isoindole-1,3(2H)-dione or pharmaceutically acceptable salts with amines RNH2 [wherein R = H, alkyl, or (un)substituted Ph], followed by further reacting with RNH2 and condensation with p-nitrophenyl 2-(furfurylsulfinyl)acetate to give Lafutidine in 85-95% yield. [on SciFinder(R)]