对甲苯磺酸索拉非尼的合成 |
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引用本文: | 赵乘有,陈林捷,许煦,罗晓燕,冀亚飞.对甲苯磺酸索拉非尼的合成[J].中国医药工业杂志,2007,38(9):614-616. |
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作者姓名: | 赵乘有 陈林捷 许煦 罗晓燕 冀亚飞 |
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作者单位: | 1. 华东理工大学药学院,上海,200237 2. 华东理工大学化工学院,上海,200237 |
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摘 要: | 吡啶甲酸经氯化、酰胺化、亲核取代得中间体4-(4-氨基苯氧基)-2-(甲基氨甲酰基)吡啶,与4-氯-3-(三氟甲基)苯异氰酸酯缩合、再成盐得对甲苯磺酸索拉非尼,总收率为64%。
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关 键 词: | 索拉非尼 抗肿瘤药 多激酶抑制剂 合成 |
文章编号: | 1001-8255(2007)09-0614-03 |
修稿时间: | 2007-06-04 |
Synthesis of Sorafenib Tosylate |
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Authors: | ZHAO Cheng-you CHEN Lin-jie XU Xu LUO Xiao-yan JI Ya-fei |
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Institution: | 1. School of Pharmacy; 2. College of Chemical Engineering, East China University of Science and Technology, Shanghai 200237 |
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Abstract: | Sorafenib tosylate was synthesized from 2-picolinic acid by chlorination,amidation,nucleophilic substitution to obtain 4-(4-aminophenoxy)-2-(methylcarbamoyl)pyridine,which was subjected to condensation with 4-chloro-3-(trifluoromethyl)phenylisocyanate and salt formation with an overall yield of 64%. |
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Keywords: | sorafenib antitumor multikinase inhibitor synthesis |
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