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| 卡立泊来德的合成工艺改进 | |
| 引用本文： | 金宁,徐云根,华维一. 卡立泊来德的合成工艺改进[J]. 中国药物化学杂志, 2006, 16(2): 112-113 |
| 作者姓名： | 金宁 徐云根 华维一 |
| 作者单位： | 中国药科大学,新药研究中心,江苏,南京,210009 |
| 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。 |
| 关 键 词： | 药物化学 工艺改进 化学合成 卡立泊来德 |
| 文章编号： | 1005-0108（2006）02-0112-02 |
| 收稿时间： | 2005-06-01 |
| 修稿时间： | 2005-06-01 |
Improved synthesis of cariporide |
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| JIN Ning,XU Yun-gen,HUA Wei-yi. Improved synthesis of cariporide[J]. Chinese Journal of Medicinal Chemistry, 2006, 16(2): 112-113 | |
| Authors: | JIN Ning XU Yun-gen HUA Wei-yi |
| Affiliation: | Center of Drug Discovery, China Pharmaceutical University, Nanjing 210009, China |
| 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. |
| Keywords: | medicinal chemistry process improvement chemical sy nthesis cariporide |
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