PROCESS FOR THE PREPARATION OF 2-(R)-(1- (R)-(3,5-BIS (TRIFLUOROMETHYL) PHENYL)ETHOXY) -4-((5-DIMETHYLAMINOMETHYL) -1,2,3-TRIAZOL -4-YL)METHYL) -3-(S)-(4- FLUOROPHENYL) MORPHOLINE

摘要

The present invention is directed to the compound 4-N,N-dimethylaminomethyl -5-formyl-1, 2,3 -triazole (I) which is a valuable intermediate in a novel convergent process for the preparation of 2-(R)-(1- (R)-(3,5-bis (trifluoromethyl) phenyl)-ethoxy) -4-(5-(dimethylamino) methyl-1,2,3-triazol -4-yl)methyl) -3-(S)-(4- fluorophenyl) morpholine (II) which is a potent and selective substance P (or neurokinin-1) receptor antagonist useful as a therapeutic agent.