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| 瑞舒伐他汀中间体的合成工艺 |
| Synthesis process for Rosuvastatin intermediates |
| 投稿时间：2026-03-17 修订日期：2026-04-13 |
| DOI： |
| 中文关键词: 瑞舒伐他汀 工艺优化 胆固醇 合成路线 |
| 英文关键词: rosuvastatin process optimization cholesterol synthetic route |
| 基金项目:国家自然科学(No. 22105150)； |
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| 摘要点击次数: 31 |
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| 中文摘要: |
| 瑞舒伐他汀类药物是一类治疗胆固醇的药物,(4R,6S)-6-[(乙酰氧)甲基]-2,2-二甲基-1,3-二氧六环-4-乙酸叔丁酯作为瑞舒伐他汀重要的一种中间体。本文介绍一种基于酶法得到的(4R,6S)-6-(氯甲基)四氢-2H-吡喃-2,4-二醇为起始原料,经过四步反应得到中间体(4R,6S)-6-[(乙酰氧)甲基]-2,2-二甲基-1,3-二氧六环-4-乙酸叔丁酯的方法。该方法合成路线简单,原料易得,且反应条件温和。 |
| 英文摘要: |
| Rosuvastatin is a class of drugs for the treatment of cholesterol, and (4R,6S)-tert-butyl (4R,6S)-6-[(acetyloxy)methyl]-2,2-dimethyl-1,3-dioxane-4-acetate serves as an important kind of intermediate for Rosuvastatin. In this paper, we present a method to synthesize intermediate (4R,6S)-6-[(acetyloxy)methyl]-2,2-dimethyl-1,3-dioxane-4-acetate by using enzyme-based intermediate (4R,6S)-6-(chloromethyl)tetrahydro-2H-pyran-2,4-diol through a four-step procedure. The method is characterized by a simple synthesis route, easy availability of raw materials and mild reaction conditions. |
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