| 匹伐他汀钙中间体的合成工艺改进 |
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| 引用本文： | 单继雷,汤旗,李志裕,倪春峰,李睿婷,侯仲轲. 匹伐他汀钙中间体的合成工艺改进[J]. 精细化工中间体, 2008, 38(5) |
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| 作者姓名： | 单继雷 汤旗 李志裕 倪春峰 李睿婷 侯仲轲 |
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| 作者单位： | 浙江国邦药业有限公司,浙江,上虞,312369;中国药科大学,江苏,南京,210009 |
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| 摘 要： | 以L-(-)苹果酸为起始原料,经甲酯化、硼烷选择性还原、三苯甲基保护、克莱森酯缩合、立体选择性还原、缩酮保护、脱三苯甲基保护、斯文氧化制得匹伐他汀钙重要中间体(3R,5S)-3,5-二羟基-6-氧代-3,5-O-亚异丙基己酸叔丁酯,收率为21.2%。降低了生产成本,提高了收率,更适合于工业化生产。
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| 关 键 词： | 匹伐他汀钙 L-(-)苹果酸 合成 |
An Improvement in Synthesis of Intermediate of Pitavastatin Cacium |
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| SHAN Ji-lei,TANG Qi,LI Zhi-yu,NI Chun-fen,LI Rui-ting,HOU Zhong-ke. An Improvement in Synthesis of Intermediate of Pitavastatin Cacium[J]. Fine Chemical Intermediates, 2008, 38(5) |
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| Authors: | SHAN Ji-lei TANG Qi LI Zhi-yu NI Chun-fen LI Rui-ting HOU Zhong-ke |
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| Affiliation: | SHAN Ji-lei1,TANG Qi1,LI Zhi-yu2,NI Chun-feng2,LI Rui-ting1,HOU Zhong-ke1(1.Zhejiang Guobang Pharmaceutical Co.,LTD,Shangyu 312369,2.China Pharmaceutical University,Nanjing 210009,China) |
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| Abstract: | This method is improved for preparing the intermediate of pitavastatin calcium by the reaction of L-(-)-malic acid through methyl esterification,selective reduction,trityl protection,Claisen condensation,stereoselective reduction,ketalization,deprotection of trityl and Swern oxidation.The total yield is 21.2%.This method reduced the production cost,enhanced yield,and suits for industrial production. |
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| Keywords: | pitavastatin calcium L-(-)-malic acid synthesis |
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