| 对甲苯磺酸索拉非尼的合成 |
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| 引用本文： | 杨欣,唐家邓,岑均达.对甲苯磺酸索拉非尼的合成[J].中国医药工业杂志,2012(7):521-524. |
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| 作者姓名： | 杨欣 唐家邓 岑均达 |
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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,创新药物与制药工艺国家重点实验室,上海200437 |
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| 基金项目： | 国家"重大新药创制"科研重大专项 |
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| 摘 要： | 4-氯-3-三氟甲基苯胺(5)和氯甲酸苯酯反应得到4-氯-3-(三氟甲基)苯基]氨基甲酸苯酯(6),再和对氨基苯酚缩合得到N-4-氯-3-(三氟甲基)苯基]-N-(4-羟基苯基)脲(7)。另用2-吡啶甲酸(2)经氯化、酰胺化得中间体N-甲基-(4-氯-2-吡啶基)甲酰胺(4)。4和7经亲核取代及成盐反应制得对甲苯磺酸索拉非尼,总收率约62%(以5计)。
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| 关 键 词： | 索拉非尼 抗肿瘤药 合成 |
Synthesis of Sorafenib Tosylate |
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| Authors: | YANG Xin TANG Jiadeng CEN Junda |
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| Institution: | (State Key Lab.of New Drug & Pharmaceutical Process,Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry,Shanghai 200437) |
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| Abstract: | N-4-Chloro-3-(trifluoromethyl) phenyl]-N-(4-hydroxyphenyl) urea(7) was prepared from 4-chloro- 3-(trifluoromethyl) aniline by reaction with phenyl chloroformate and condensation with 4-aminophenol.Meanwhile, N-methyl-(4-chloropyridin-2-yl) carboxamide(4) was prepared from 2-picolinic acid(2) by chlorination and amidation. Sorafenib tosylate was synthesized from 4 and 7 by condensation and salt formation with an overall yield of about 62% based on 4-chloro-3-(trifluoromethyl) aniline]. |
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| Keywords: | sorafenib antitumor agent synthesis |
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