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抗肿瘤药物舒尼替尼的新合成方法 被引量：3

A new synthesis of antitumor agent sunitinib
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摘要 目的研究抗肿瘤药物舒尼替尼的新合成路线。方法以4-氟-2-碘苯胺(3)为原料,经氯乙酰化、膦酰化、Horner-Emmons-Wittig反应得N-[2-(二乙胺基)乙基]-5-[(E)-2-(4-氟-2-碘代-苯胺基甲酰基)-乙烯基]-2,4-二甲基-1H-吡咯-3-甲酰胺(6);6在醋酸钯和三乙胺的作用下,通过分子内5-exo型环合反应得舒尼替尼。结果与结论新中间体及舒尼替尼结构经核磁共振谱和质谱确证,合成路线未见报道。 Aim To explore a novel protocol for the synthesis of antitumor agent sunitinib.Methods Starting from 2-iodo-4-fluoroaniline（3）,5-[2-（4-fluoro-2-iodo-phenylcarbamoyl）-vinyl]-2,4-dimethyl-1H-pyrrole-3-carboxylic acid（2-diethylamino-ethyl）-amide（6） was obtained via chloroacylation,phosphonation and Horner-Emmons-Wittig reaction.Sunitinib（1） was obtained by intramolecular 5-exo-type annulation reaction in the presence of Pd（OAc）2 and Et3N.Results and conclusion The novel intermediates and target compound were identified by NMR and MS spectra,and the process has not been disclosed before.
作者 陈云华 周旭荣 白骅
机构地区 浙江省台州职业技术学院生物与化学工程系 浙江海正药业股份有限公司
出处 《中国药物化学杂志》 CAS CSCD 2010年第2期99-101,共3页 Chinese Journal of Medicinal Chemistry
关键词 化学合成 舒尼替尼 抗肿瘤药物 环合反应 chemical synthesis sunitinib antitumor agent annulation
分类号 R914 [医药卫生—药物化学]
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参考文献12

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中国药物化学杂志
2010年 第2期

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