Author(s): LI Yan-yang, ZHAO Yan-jin, LI Shu-xin, Institute of Radiation Medicine, Academy of Military Medical Sciences
Pages: 2090-2092
Year: 2013 Issue:  17
Journal: Chinese Journal of New Drugs
Keyword:  Hh信号通路抑制剂; vismodegib; 合成;
Abstract: 目的:合成Hh通路抑制剂vismodegib。方法:以2-氯-5-硝基苯胺为起始原料通过4步反应合成了Hh通路抑制剂vismodegib(2-氯-N-(4-氯-3-(吡啶-2-基)苯基)-4-(甲磺酰基)苯甲酰胺)。结果与结论:目标产物结构经1H-NMR和ESI-MS确证,总收率为51.11%。此路线制备工艺反应条件温和且原料易得,后处理简单,适合于小规模制备的实验室研究。