(2S,4S)-1-(4-硝基苄氧羰基)-2-[(3-烯丙氧羰基)-苯基氨基甲酰基]-吡咯烷-4-基硫醇的合成工艺改进

Improvement on the synthesis of(2S,4S)-1-(4-nitrobenzy-loxycarbonyl)-2-[(3-allyloxycarbonyl)-benziaminocarbonyl] pyrrolidine-4-mercaptan

采用价格低廉的反-4-羟基-L-脯氨酸为原料,通过7步反应,制备尔他培南的关键中间体———标题化合物,总收率37%。原料来源方便,成本低,而且减少了毒害作用,增加了安全性,适宜于工业化生产。

（ 2S, 4S ）-1-（ 4-nitrobenzyloxycarbonyl ）-2-[ （ 3-ally- loxycarbonyl）-benziaminocarbonyl ] pyrrolidine-4-mereaptan was prepared by using the inexpensive trans-4-hydroxyl-L-proline as the original material via seven steps of reactions to give an overall yield of 37 %. This method is environmentally friendly and more suitable for commercialization.