Process for the preparation of oxazaphosphorine-2-amines

摘要

A process for the preparation of oxazaphosphorine-2-amines of the formula (I) described by the reaction schemein which R1 is H, 2-bromoethyl, 2-chloroethyl, 2-hydroxyethyl, 2-mesyloxyethyl or 1-phenylethyl; R2 is H or 2-chloroethyl; R3 is H, 2-bromoethyl, 2-chloroethyl or 1-phenylethyl; and R4 is H; or R1 and R2, and also R3 and R4, together with the linked N atom, form an aziridide ring, where R1, R2 and R3 are not simultaneously H, and R1 and R3 are not simultaneously 1-phenylethyl; and Y, which is optionally present, is hydrogen chloride or hydrogen bromide. The reaction is carried out in a single vessel with phosphoryl chloride and an auxiliary base as an acid-binding agent with minimization of the effect of water and without isolation of an intermediate compound.