| 舒尼替尼的合成 |
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| 引用本文： | 刘彪,林蓉,廖健宇,李子成,陈珂磊. 舒尼替尼的合成[J]. 中国医药工业杂志, 2007, 38(8): 539-542 |
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| 作者姓名： | 刘彪 林蓉 廖健宇 李子成 陈珂磊 |
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| 作者单位： | 四川大学化工学院制药与生物工程系,四川成都,610065 |
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| 摘 要： | 乙酰乙酸乙酯经Knorr反应、水解脱羧、甲酰化、水解、酰胺化得N-（2-二乙胺基乙基）-2,4-二甲基-5-甲酰基-1H-吡咯-3-甲酰胺（8）;另以对氟苯胺、水合氯醛和盐酸羟胺经羰基化、环合、还原得5-氟-1,3-二氢吲哚-2-酮（13）。8和13在三乙胺存在下缩合得抗肿瘤药舒尼替尼,总收率约13%（以乙酰乙酸乙酯计）。
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| 关 键 词： | 舒尼替尼 抗肿瘤药 合成 |
| 文章编号： | 1001-8255（2007）08-0539-04 |
| 修稿时间： | 2007-04-02 |
Synthesis of Sunitinib |
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| LIU Biao,LIN Rong,LIAO Jian-yu,LI Zi-cheng,CHEN Ke-lei. Synthesis of Sunitinib[J]. , 2007, 38(8): 539-542 |
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| Authors: | LIU Biao LIN Rong LIAO Jian-yu LI Zi-cheng CHEN Ke-lei |
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| Affiliation: | Dept. of Pharmaceutical and Biological Engineering, College of Chemical Engineering, Sichuan University, Chengdu 610065 |
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| Abstract: | N-(2-Diethylaminoethyl)-2,4-dimethyl-5-formyl-1H-pyrrole-3-carboxamide(8) was synthesized from ethyl acetoacetate via Knorr reaction,hydrolysis,decarboxylation,formylation,hydrolysis and then amidation. Sunitinib was synthesized form compound 8 and 5-fluoro-1,3-dihydroindol-2-one(13) by condensation in presence of Et3N with an overall yield of about 13%(based on ethyl acetoacetate). Compound 13 was prepared from p-fluoroaniline,chloral hydrate and hydroxylamine hydrochloride by carbonylation,cyclization and reduction. |
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| Keywords: | sunitinib antitumor agent synthesis |
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