Cabozantinib(S)-苹果酸盐的合成工艺研究

The study on Synthetic Technology of Cabozantinib (S)-malate

以3,4-二甲氧基苯乙酮为原料,经硝化、缩合、环合、氯代和取代等多步反应合成了用于不可手术切除的局部晚期或转移性甲状腺髓样癌的治疗的目标产物Cabozantinib(S)-苹果酸盐。该路线所用的原料价廉易得、反应条件温和、操作简单、收率较高。

The Cabozantinib （S）-malate, which was used for the treatment of locally advanced or metastatic progressive medullary thyroid cancer, was prepared from 3,4-dimethoxyacetophenone by nitration, condensation, cyclization, chlorination and substitution, etc. In this synthetic route, raw materials were commercially available, reactive conditions were mild, the operation was easy, and the yield was higher.