| 酒石酸拉索昔芬的合成 |
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| 引用本文： | 童玲,朱雪焱,袁哲东. 酒石酸拉索昔芬的合成[J]. 中国医药工业杂志, 2011, 42(7) |
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| 作者姓名： | 童玲 朱雪焱 袁哲东 |
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| 作者单位： | 中国医药工业研究总院上海医药工业研究院,上海,200437 |
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| 基金项目： | 国家“重大新药创制”科技重大专项(2009ZX09301-007) |
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| 摘 要： | 6-甲氧基-1-四氢萘酮与1-[2-(4-溴苯氧基)乙基]吡咯烷缩合后,经三溴化吡啶鎓溴代,与苯硼酸进行Suzuki偶合、钯炭催化加氢、48%氢溴酸脱甲基后,经D-酒石酸拆分成盐得酒石酸拉索昔芬,总收率约15%[以1-[2-(4-溴苯氧基)乙基]吡咯烷计]。
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| 关 键 词： | 酒石酸拉索昔芬 抗骨质疏松药 合成 |
Synthesis of Lasofoxifene Tartrate |
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| TONG ling,ZHU Xueyan,YUAN Zhedong. Synthesis of Lasofoxifene Tartrate[J]. , 2011, 42(7) |
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| Authors: | TONG ling ZHU Xueyan YUAN Zhedong |
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| Affiliation: | TONG ling,ZHU Xueyan,YUAN Zhedong~* (Shanghai Institute of Pharmaceutical Industry,China State Institute of Pharmaceutical Industry,Shanghai 20043 7) |
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| Abstract: | 6-Methoxy-1-tetralone was condensed with 1-[2-(4-bromophenoxy)ethyl]pyrrolidine,followed by bromination with pyridinium bromide perbromide,coupling with phenylboronic acid,reduction with H_2 over Pd/C, demethylation with 48%hydrobromic acid and then resolution with D-tartaric acid to obtain lasofoxifene tartrate.The overall yield was about 15%[based on 1-[2-(4-bromophenoxy) ethyl]pyrrolidine]. |
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| Keywords: | lasofoxifene tartrate anti-osteoporosis drug synthesis |
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