155435-45-3Relevant articles and documents
Everolimus intermediate, and preparation method and application thereof
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Paragraph 0073; 0074; 0075; 0076; 0077; 0078, (2019/06/13)
The invention discloses an everolimus intermediate, and a preparation method and an application of the everolimus intermediate. A structure of the everolimus intermediate C is shown as formula (1) asshown in the specification. The preparation method comprises the following step: allowing 28-monosilicon protected rapamycin (an everolimus intermediate B) to react with trifluoromethanesulfonic acidsingle-protection glycol ester in the presence of organic base. The invention further discloses the application of the everolimus intermediate C. The preparation method of the everolimus intermediateis simple and high in yield; everolimus prepared from the intermediate can reduce side reactions; a technical operation procedure is simplified; the total yield is increased; the product quality is ensured; and therefore, the preparation method has better industrial application and popularization prospects.
METHOD FOR PREPARING 42-(DIMETHYLPHOSPHINATE) RAPAMYCIN
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, (2014/03/24)
A method for preparing 42-(dimethylphosphinate) Rapamycin (Ridaforolimus) (I) is provided, which has advantages of high conversion rate and no 31,42-bis(dimethyl phosphinate) Rapamycin (III) generated. In the method of the present invention, Rapamycin (II) is firstly reacted with triethyl chlorosilane in a base condition to form 31,42-bis(triethylsilylether) Rapamycin (IV-b), followed by a selective deprotection process to obtain 31-triethylsilylether Rapamycin (V-b). Next, a phosphorylation reaction is performed by using dimethylphosphinic chloride under a base solution to obtain a crude product. Finally, a deprotection reaction is performed in a diluted sulfuric acid solution to obtain a crude product of Ridaforolimus (I). Since the conversion rate of each step of the method of the present invention is higher than 98%, it indicates that the method of the present invention is suitable for industrial production.
Manipulation of the C(22)-C(27) region of rapamycin: Stability issues and biological implications
Nelson, Frances C.,Stachel, Shawn J.,Eng,Sehgal, Suren N.
, p. 295 - 300 (2007/10/03)
A novel series of rapamycin derivatives with modifications in the C(22)- C(27) region has been prepared. These compounds are evaluated for their ability to prevent ring fragmentation while still retaining immunosuppressive capabilities.