抗癌新药依维莫司的合成工艺优化和抗癌活性研究

Development of New Synthetic Process of Everolimus,A New Anticancer Drug and Its Anticancer Evaluation in Vitro

依维莫司(Everolimus)为西罗莫司衍生物,在肿瘤治疗领域使用较为广泛。目前,现有依维莫司制备工艺产率低,成本高,对其合成进行研究有重要意义。本研究以西罗莫司为原料经过两步化学半合成得依维莫司终产品,总收率达63%,获得较优的生产工艺,为后期工业化生产奠定技术基础。最后,通过体外抗肿瘤活性检测,本研究获得的自制依维莫司具有与商购依维莫司相当的抗肾细胞癌活性。

Everolimus,as a derivative of sirolimus,which is widely employed in the field of tumor clinical treatment.presently,the reported synthetic process of everolimus was with low yield and high cost.There,it is of great significance to optimized the synthetic process.In this study,everolimus is prepared from sirolimus via two-step reactions,with an overall yield of 63%,and a better synthetic process is obtained,which lays a technical foundation for later industrial production.Finally,The antitumor activity was detected in vitro,the anti-cancer activity of everolimus prepared in this study was comparatively with that of commercial everolimus.