2-[二-(2-氯乙基)-胺基]-5-苄氧基-1,3,2-氧氮磷杂环己烷-2-氧化物的不对称合成

Asymmetric Synthesis of 2-(Bis-(2-Chloroethyl)-Amino)-5- Benzyloxytetrahydro-2H-1, 3,2-Oxazaphosphorine-2-Oxide

2-[二-(2-氯乙基)-胺基]-5-苄氧基-1,3,2-氧氮磷杂环己烷-2-氧化物是抗癌药物Endoxan的衍生物,其光学异构体的合成已有报道.本文报道了我们从廉价易得的手性原料天然-L-酒石酸开始,通过较为简捷的合成路线,完成了对目标化合物全部4个光学异构体的合成.化合物的有关数据参见表1.

A novel synthetic route of all enantiomers of 2-(bis-(2-chloroethyl)-amino)-5-benzy-loxy-tetrahydro-2H-1,3,2-oxazaphosphorine-2-oxide starting from the natural L-tartaric acid as a chiral synthon is described. The results relating to the structures of the intermediates and products in this synthesis are discussed.