331810-10-7Relevant articles and documents
Synthesis and anticancer activity of novel rapamycin C-28 containing triazole moiety compounds
Huang, Qingwen,Xie, Lijun,Chen, Xiaoming,Yu, Hui,Lv, Yubing,Huang, XueHui,Ying, Jiayin,Zheng, Congshen,Cheng, Yuanrong,Huang, Jie
, (2018)
Rapamycin is an mTOR allosteric inhibitor with multiple functions such as immunosuppressive, anticancer, and lifespan prolonging activities. Its C-43 semi-synthetic derivatives temsirolimus and everolimus have been used as mTOR targeting anticancer drugs
Preparation method of everolimus
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, (2019/06/13)
The invention discloses a preparation method of everolimus. The preparation method comprises the following step of performing deprotection reaction on an everolimus intermediate C. The preparation method of everolimus adopts a manner of regioselective protection of rapamycin 28-hydroxyl, so that the selectivity of a 40-hydroxyl alkylation reaction is improved; side reactions are reduced; a total yield of everolimus calculated from rapamycin can reach above 70%; compared with yields reported in available literatures, the yield is greatly increased; a technical operation procedure is simplified;the product quality is ensured; and the preparation method has better industrial application and popularization prospects.
Intermediate of temsirolimus and preparation method thereof
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, (2019/01/06)
The invention provides an intermediate of temsirolimus. The intermediate has better selectivity and higher yield when used for preparation of the temsirolimus. The intermediate provided by the invention has a structural formula which is described in the specification.