| 摘要 |
This invention discloses a solvent-free process for the preparation of cyclophosphamide. According to this invention, there is no solvent used during the reaction step for preparing cyclophosphamide, so that the total volume of the reaction for preparing cyclophosphamide can be reduced and the manufacture of cyclophosphamide can become more efficient. Furthermore, the above solvent-free process for the preparation of cyclophosphamide is more simply operated, more economic, and more environmental friendly than the preparation of cyclophosphamide in the prior art. |
| 主权项 |
1. A solvent-free process for the preparation of cyclophosphamide, wherein the reaction step of the solvent-free process does not use solvent, comprising:
reacting a phosphoryl chloride, a bis(2-chloroethyl)amine hydrochloride, a 3-aminopropanol, and a base, including the steps of:
reacting one of said amines of said bis(2-chloroethyl)amine hydrochloride and 3-aminopropanol with phosphoryl chloride in the presence of said base to form an intermediate; andreacting said intermediate with another of said amines not used in the above step to form the cyclophosphamide, wherein said phosphoryl chloride, said bis(2-chloroethyl)amine hydrochloride, said 3-aminopropanol, said base, and said cyclophosphamide are represented as the following formula: wherein G is selected from group consisting of the following: N, O, R7 is selected from the group consisting of the following: C1-C3 straight-chain alkyl group, C1-C3 branched alkyl group, when G is N, R8 is selected from the group consisting of the following: C1-C3 straight-chain alkyl group, C1-C3 branched alkyl group. |
