| 唐振权,莫卫民,沈振陆,孙楠,胡宝祥,胡信全.DDQ/TBN催化分子氧氧化芳构化合成罗素伐他汀母核中间体[J].分子催化,2012,(3):211-215 |
| DDQ/TBN催化分子氧氧化芳构化合成罗素伐他汀母核中间体 |
| The Study of the Synthesis of Rosuvastatin Intermediate via DDQ/TBN Catalyzed Aerobic Oxidative Aromatization |
| 投稿时间：2012-04-06 修订日期：2012-05-09 |
| DOI： |
| 中文关键词: 罗素伐他汀中间体 氧化芳构化 二氢嘧啶 嘧啶 DDQ 氧气 |
| 英文关键词:Rosuvastatin intermediate Oxidative aromatization Dihydro-pyrimidine Pyrimidine DDQ molecular oxygen |
| 基金项目:国家自然科学基金项目（21146001） |
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| 中文摘要: |
| 以DDQ和TBN为催化剂，氧气为氧源，研究了罗素伐他汀母核合成过程中从多取代二氢嘧啶（I）转化为相应的嘧啶中间体（II）的氧化芳构化反应。考察了反应温度，反应溶剂及催化剂用量对氧化芳构化反应的影响。优化实验结果表明，以2 mol%的DDQ及10 mol% TBN为催化剂，氧气为氧源，在甲苯中60 oC反应24小时，多取代二氢嘧啶完全转化，获得高选择性的氧化芳构化产物嘧啶中间体（II）。在50 mmol规模的氧化芳构化反应的实验中获得了98.8%的分离收率，反应的后处理方便简洁。 |
| 英文摘要: |
| A new catalytic system composed with DDQ/TBN for conversion of multi-substituted dihydro-pyrimidine (I) to Rosuvastatin pyrimidine intermediate via aerobic aromatization has been developed. The effects of reaction temperature, solvent and catalyst loading have been fully investigated on the aerobic oxidative aromatization. The optimal aerobic oxidation conditions for the quantitative conversion of multi-substituted dihydro-pyrimidine (I), together with high selectivity of desired pyrimidine (II), was obtained with 2 mol% of DDQ, 10 mol% of TBN in toluene under 60 oC for 24 h. Up to 98.8% of isolated yield of the desired product was achieved in a 50 mmol scale through very simple work-up procedure. |
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