| HMG-CoA还原酶抑制剂中间体合成新工艺 |
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| 引用本文： | 王文金,石炜,徐勤耀,杨琍苹. HMG-CoA还原酶抑制剂中间体合成新工艺[J]. 有机化学, 2008, 28(4): 663-666 |
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| 作者姓名： | 王文金 石炜 徐勤耀 杨琍苹 |
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| 作者单位： | 华东师范大学化学系,上海,200062 |
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| 摘 要： | (3R,5S)-6-羟基-3,5-O,O-亚异丙基-二羟基己酸叔丁酯是制备HMG-CoA还原酶抑制剂的重要结构单元, 提出了通过两次不对称催化氢化在温和的条件下方便高效高立体选择性合成(3R,5S)-6-羟基-3,5-O,O-亚异丙基-二羟基己酸叔丁酯的新工艺. 该工艺8步总产率38%, de值99%.
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| 关 键 词： | 对映选择性氢化 保护基 工业化 |
| 收稿时间： | 2007-01-05 |
| 修稿时间： | 2007-01-05 |
New Process for a Pivotal Intermediate of the HMG-CoA Reductase Inhibitors |
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| WANG Wen-Jin,SHI Wei,XU Qin-Yao,YANG Li-Ping. New Process for a Pivotal Intermediate of the HMG-CoA Reductase Inhibitors[J]. Chinese Journal of Organic Chemistry, 2008, 28(4): 663-666 |
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| Authors: | WANG Wen-Jin SHI Wei XU Qin-Yao YANG Li-Ping |
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| Affiliation: | (Department of Chemistry, East China Normal University, Shanghai 200062) |
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| Abstract: | A new process was described for the preparation of t-butyl (3R,5S)-6-hydroxy-3,5-O,O-isopropylidenedioxyhexanoate, which is a key intermediate for a number of HMG-CoA reductase inhibitors. The intermediate was easily and efficiently obtained under mild reaction conditions via two enantioselective hydrogenation reactions with a high di-astezeoselectivity of 99% de in an overall yield of 38% for the eight-step procedure. |
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| Keywords: | enantioselective hydrogenation protecting group industrialization |
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