PROCESS FOR THE PREPARATION OF 1,3-DIAMINOPROPANE DERIVATIVES AND INTERMEDIATES USEFUL IN THIS PROCESS

摘要

A process for the preparation of a compound of formula (B), or an addition salt and/or a solvate thereof, wherein Ra and Rd are independently phenyl optionally substituted by one, two or three of halogen, trifluoromethyl, C1-4 alkoxy, C1-4 alkyl, cyano, hydroxy, nitro, NReRf or O2SNReRf wherein Re and Rf are independently hydrogen or C1-6 alkyl or together are C3-6 polymethylene, or disubstituted at adjacent carbon atoms by C1-2 alkylenedioxy and optionally further substituted by one of the above groups; Rc is hydrogen or C1-4 alkyl; A represents C3 alkylene; and B represents C1-4 alkylene; which process comprises reacting a compound of the formula (VI): Ra-NH2, wherein Ra represents phenyl optionally substituted by one, two or three of halogen, trifluoromethyl, C1-4 alkoxy, C1-4 alkyl, cyano, hydroxy, nitro, NReRf or O2SNReRf wherein Re and Rf are independently hydrogen or C1-6 alkyl or together are C3-6 polymethylene, or disubstituted at adjacent carbon atoms by C1-2 alkylenedioxy and optionally further substituted by one of the above groups; with a compound of formula (VII), wherein Rd represents phenyl optionally substituted by one, two or three of halogen, trifluoromethyl, C1-4 alkoxy, C1-4 alkyl, cyano, hydroxy, nitro, NReRf or O2SNReRf wherein Re and Rf are independently hydrogen or C1-6 alkyl or together are C3-6 polymethylene, or disubstituted at adjacent carbon atoms by C1-2 alkylenedioxy and optionally further substituted by one of the above groups; Rc is hydrogen or C1-4 alkyl; and B represents C1-4 alkylene; and thereafter reducing the intermediate so formed and, optionally, forming an addition salt of the compound of formula (B) and/or a solvate thereof.