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(3R,5S)-6-氧代-3,5-二羟基-3,5-O-亚异丙基己酸叔丁酯的合成

Synthesis of t-Butyl(3R,5S)-6-oxo-3,5-O-isopropylidene-3,5-dihydroxyhexanoate
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摘要 目的设计路线合成匹伐他汀钙侧链。方法以(3R,5S)-6-乙酰氧基-3,5-二羟基-3,5-O-亚异丙基己酸叔丁酯为原料经水解、Swern氧化得匹伐他汀钙的重要中间体(3R,5S)-6-氧代-3,5-二羟基-3,5-O-亚异丙基己酸叔丁酯。结果总收率为80.8%。结论经1H-NMR确定为该化合物。 Objective To synthesize the side chain of Pitavastatin calcium.Methods t-Butyl(3R,5S)-6-oxo-3,5-O-isopropylidene-3,5-dihydroxyhexanoate,a key intermediate of pitavastatin calcium,was Synthesized from t-Butyl(3R,5S)-6-acetoxy-3,5-O-isopropylidene-3,5-dihydroxyhexanoate by hydrolysis reaction and Swern oxidation.Results The over yields of the reactions are 80.8%.Conclusion The product were identified by 1HNMR.
作者 赵焕臣 张春桃 吕延华
机构地区 湖南中医药大学 湖南中医药大学有机药化教研室 深圳市东阳光实业发展有限公司
出处 《中国现代药物应用》 2009年第6期21-22,共2页 Chinese Journal of Modern Drug Application
关键词 (3R 5S)-6-氧代-3 5-二羟基-3 5-O-亚异丙基己酸叔丁酯 水解 Swern氧化 匹伐他汀钙 中间体 t-Butyl（3R 5S）-6-oxo-3 5-O-isopropylidene-3 5-dihydroxyhexanoate Hydrolysis reaction Swern oxidation Pitavastatin calcium Intermediate
分类号 R914 [医药卫生—药物化学]
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中国现代药物应用
2009年 第6期

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