Patent ID: 6187941
Filing Date: 2001-02-13
Classification: A61P,C07F

Abstract:
A process for the preparation of oxazaphosphorine-2-amines of formula 1: ##STR4##in whichR.sub.1 is H, 2-bromoethyl, 2-chloroethyl, or 2-mesyloxyethyl;R.sub.2 is H or 2-chloroethyl; andR.sub.3 is H, 2-bromoethyl, 2-chloroethyl or 1-phenylethyl; orR.sub.1 and R.sub.2, together with the linked N atom, form an aziridine ring;said process comprising reacting a phosphoryl halide of formula 2, an amine of formula 3, and an amine of formula 4: ##STR5##in which R.sub.1, R.sub.2 and R.sub.3 have the same meanings as formula 1, R.sub.4 is H, or R.sub.3 and R.sub.4, together with the linked N atom, form an aziridine ring, X is chlorine or bromine, X only being bromine if R.sub.1 or R.sub.3 is 2-bromoethyl, and Y, which is optionally present, is hydrogen chloride or hydrogen bromide; with an auxiliary base as an acid binding agent in the presence of inert solvents without isolation of an intermediate compound;whereby, in a first step, one compound each of the formulae 2 and 3 are reacted and, in a second step, a compound of the formula 4 is reacted; or whereby, in a first step, one compound each of the formulae 2 and 4 are reacted and, in a second step, a compound of the formula 3 is reacted.