| 何灵敏, 林丰, 王璨, 陈云峰.瑞舒伐他汀中间体的合成工艺[J].海南师范大学学报自科版,2026,(2):150-154 |
| 瑞舒伐他汀中间体的合成工艺 |
| Synthesis Process for Rosuvastatin Intermediates |
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| DOI：10.12051/j.issn.1674-4942.2024.04.004 |
| 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 synthesis route |
| 基金项目:国家自然科学基金项目（22105150） |
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| 摘要点击次数: 536 |
| 全文下载次数: 8 |
| 中文摘要: |
| 瑞舒伐他汀类药物是一类治疗高脂血症和高胆固醇血症的药物，（4R，6S）-6-［（乙酰氧）甲基］-2，2-二甲基-1，3-二氧六环-4-乙酸叔丁酯是合成瑞舒伐他汀的一种重要的中间体。本文介绍一种以酶法制备的（4R，6S）-6-（氯甲基）四氢-2H-吡喃-2，4-二醇为起始原料，经过4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 hyperlipidemia and hypercholesterolemia, 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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