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【结 构 式】 
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【分子编号】48284 【品名】(5R,6S)-6-phenyl-5-[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]-5,6,7,8-tetrahydro-2-naphthalenyl acetate 【CA登记号】 |
【 分 子 式 】C30H33NO3 【 分 子 量 】455.59696 【元素组成】C 79.09% H 7.3% N 3.07% O 10.54% |
与该中间体有关的原料药合成路线共 1 条
合成路线1
该中间体在本合成路线中的序号：(II)The acetylation of racemic cis-lasofoxifene (CP-319609) (I) by conventional methods gives the corresponding acetate (II), which is submitted to an enzymatic hydrolysis with cholesterol lipase (porcine pancreas) in a pH 7 phosphate buffer to yield pure lasofoxifene with an e.e. of 96% at 35% conversion. This optical purity can be improved up to 99% e.e. by crystallization in 95:5 ethanol/water.
| 【1】 Rosati, R.L.; Liu, K.K.-C.; Yang, X.; Reinhold, A.R.; Enzyme-catalyzed asymmetric deacylation for the preparation of lasofoxifene (CP-336156), a selective estrogen receptor modulator. Org Lett 2000, 2, 25, 4025. |
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