卡立泊来德的合成工艺改进

Improved synthesis of cariporide

以对异丙基苯甲酸为原料,经过氯磺化、还原、甲基化、胍解得到卡立泊来德,总收率为45·3%。改进后的工艺路线,降低了成本,简化了操作和反应条件。

Cariporide（1）was synthesized from 4-isopropylbenzoic acid（2） as starting material. Compound 2 was treated with chlorosulfonic acid to form corresponding chlorosulfonyl defivative（3）which was reduced by sodium sulfite, followed by methytation with dimethyl sulfate to give corresponding methyl benzoate（5）. Cornpound 5 was treated with guanidine to give compound 1. The overall yield of the improved procedure is 45.3%. The process is simple and practical.