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卡立泊来德的合成工艺改进
Improved synthesis of cariporide
【摘要】 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。
【Abstract】 Cariporide was synthesized from 4-isopropylbenzoic acid(2 ) as starting material.Compound 2 was treated w ith chlorosulfonic acid to form c orresponding chlorosulfonyl derivative(3)which w as reduced by sodium sulfite,followed by methylation with dimethyl sulfate to gi ve corresponding methyl benzoate(5).Compound wa s treated with guanidine to give compound 1.The overall yield of the improved procedure is 45.3%.The process is simple and practical.
【关键词】 药物化学;
工艺改进;
化学合成;
卡立泊来德;
【Key words】 medicinal chemistry; process improvement; chemical sy nthesis; cariporide;
【Key words】 medicinal chemistry; process improvement; chemical sy nthesis; cariporide;
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2006年02期
- 【分类号】TQ463
- 【下载频次】169