PROCESS AND INTERMEDIATE COMPOUNDS FOR THE PREPARATION OF (1R, 2S, 5S) -3-AZABICICLO (3,1,0) HEXANO-2-CARBOXAMIDA, N- (3-AMINO-1- (CICLOBUTILMETIL) -2,3-DIOXOPROPIL ) -3 - ((2S) -2 - (((1,1-DIMETHYTILE) AMINO) CARBONYLAMINE) -3,3-DIMETHYL-1-OXOBUTIL) -6,6-DIMETHYL

摘要

A process for the preparation of a compound of the formula I comprising: (See formula) (1) coupling a compound of the formula II with a compound of the formula III to obtain a compound of the formula IV: (See formula) in where Z + represents the cation of an amine or metal, and R is selected from the group consisting of alkyl, aryl and aralkyl; (2) oxidize the hydroxyl group of a compound of the formula V to obtain a compound of the formula VI: (See formula) wherein P represents a protective group of N; (3) deprotect the compound of the formula VI to obtain a compound of the formula VII: (See formula) (4) generate a free acid compound of the formula VIII from the compound of the formula IV: (See formula) ( 5) coupling the compound of the formula VII with a compound of the formula VIII to obtain the compound of the formula I: (See formula)