| 摘要 |
The present invention relates to a method for preparing oxazaphosphorin-2-amines of the general formula (1), wherein R1 may represent H, 2-bromethyl, 2-chlorethyl, 2-hydroxyethyl, 2-mesyloxyethyl or 1-phenylethyl, R2 may represent H or 2-chlorethyl, R3 may represent H, 2-bromethyl, 2-chlorethyl or 1-phenylethyl and R4 may represent H. R1 and R2 as well as R3 and R4 may also form together with the linked N-atom a cyclic aziridin compound with the proviso that R1, R2 and R3 cannot represent simultaneously H and that R1 and R3 cannot represent simultaneously 1-phenylethyl. Y represent hydrogen hydrochloride or bromide or nothing. The compounds obtained using this new method are known drugs such as cyclophosphamide and ifosfamide which are used as cytostatic or immuno-suppressing agents. The amines (2) and (3) used as starting compounds are reacted during a single-vessel reaction with phosphoryl chloride and with an additional base used as an acid-fixation agent such as pyridine, triethylamine or alkaline or earth-alkaline carbonates. The reaction is carried out in the presence of inert solvents while reducing to a minimum the influence of water and without isolating an intermediate compound. |
