331810-13-0Relevant articles and documents
Selective substitution of 31/42-OH in rapamycin guided by an in situ ir technique
Cao, Shuang,Zhou, Xinbo,Yang, Yuanshuai,Zhong, Wu,Sun, Tiemin
, p. 7770 - 7784 (2014)
An in situ IR technique was applied in the selective synthesis of the key intermediate for rapamycin derivatives, which made the reaction endpoint easily defined. This technology solved a bothersome problem in the preparation of rapamycin derivatives, and
Preparation method of everolimus
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Paragraph 0059-0064, (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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Paragraph 0019; 0036; 0037; 0039; 0040; 0042; 0043; 0046, (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.