| (R)-比卡鲁胺的合成 |
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| 引用本文： | 沈佳其,施振华,宁奇.(R)-比卡鲁胺的合成[J].中国医药工业杂志,2006,37(2):73-75. |
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| 作者姓名： | 沈佳其 施振华 宁奇 |
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| 作者单位： | 上海医药工业研究院,上海,200437 |
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| 摘 要： | 甲基丙烯酰氯与手性助剂D-脯氨酸经酰胺化、溴化、水解得到（R）-（＋）-3-溴-2-羟基-2-甲基丙酸，酰氯化后相继与4-氰基-3-三氟甲基苯胺及4-氟苯硫酚缩合、氧化得到（R）-比卡鲁胺。总收率26％。
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| 关 键 词： | (R)-比卡鲁胺 抗前列腺癌药物 非甾体雄激素拮抗剂 手性合成 |
| 文章编号： | 1001-8255（2006）02-0073-03 |
| 收稿时间： | 2005-07-14 |
| 修稿时间： | 2005-07-14 |
Synthesis of (R)-Bicalutamide |
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| Authors: | SHEN Jia-Qi SHI Zhen-Hua NING Qi |
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| Institution: | Shanghai Institute of Pharmaceutical Industry, Shanghai 200437 |
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| Abstract: | (R)-Bicalutamide was synthesized from methyl acryloyl chloride via amidation with chiral reagent D-proline, bromination and hydrolysis to give the key intermediate (R)-(+)-3-bromo-2-hydroxy-2-methylpropanoic acid, whichafter chlorination was subjected to successive condensations with 4-cyano-3-(trifluoromethyl)aniline and 4-fluorothiophenolfollowed by oxidation with m-chloroperoxybenzoic acid with an overall yield of 26%. |
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| Keywords: | (R)-bicalutamide antiprostate cancer nonsteroidal antiandrogen chiral synthesis |
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