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新型吡咯并[2,1-f][1,2,4]三嗪酪氨酸激酶抑制剂的设计与合成
引用本文:徐中轩,蒋达洪,陈元伟.新型吡咯并[2,1-f][1,2,4]三嗪酪氨酸激酶抑制剂的设计与合成[J].合成化学,2009,17(3).
作者姓名:徐中轩  蒋达洪  陈元伟
作者单位:1. 中国科学院,成都有机化学研究所,不对称合成与手性技术四川省重点实验室,四川,成都,610041;中国科学院,研究生院,北京,100049
2. 中国科学院,成都有机化学研究所,不对称合成与手性技术四川省重点实验室,四川,成都,610041
摘    要:以对甲基苯磺酰甲基异腈和反-2-丁烯酸甲酯为原料,经过11步反应合成了7个4,5,6-三取代的新型吡咯并2,1-f]1,2,4]三嗪酪氨酸激酶抑制剂,总收率3.2%~10.0%,其结构经1H NMR和MS 表征.

关 键 词:酪氨酸激酶抑制剂  三嗪  设计  药物合成

Design and Synthesis of Novel Pyrrolo[2,1-f][1,2,4] triazines as Tyrosine Kinase Inhibitor
XU Zhong-xuan,JANG Da-hong,CHENG Yuan-wei.Design and Synthesis of Novel Pyrrolo[2,1-f][1,2,4] triazines as Tyrosine Kinase Inhibitor[J].Chinese Journal of Synthetic Chemistry,2009,17(3).
Authors:XU Zhong-xuan  JANG Da-hong  CHENG Yuan-wei
Institution:1. Key Laboratory of Asymmetric Synthesis and Chirotechnology of Sichuan Province;Chengdu Institute of Organic Chemistry;Chinese Academy of Sciences;Chengdu 610041;China;2. Graduate University of Chinese Academy of Sciences;Beijing 100049;China
Abstract:Seven novel 4,5,6-trisubtituted pyrrolo2,1-f]1,2,4]triazines as tyrosine kinase inhibitors in total yileds of 3.2%~10.0% were synthesized from tosylmethyl isocyanide and trans-2-butenic acid methyl ester by a eleven-step reaction. The structures were characterized by 1H NMR and MS.
Keywords:tyrosine kinase inhibitor  triazine  design  drug synthesis  
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