发明名称 REGIOSELECTIVE ACYLATION OF RAPAMYCIN AT C-42 POSITION
摘要 FIELD: chemistry.SUBSTANCE: invention relates to a method of producing a compound of formula (III) by selective acylation of rapamycin in 42 position using an acylation reagent of formula (I), in which Rand Rdenote residue ketal residue of formula II, in presence of a base, which is pyridine, optionally in presence of an additional solvent S, as well as a method for synthesis of temsirolimus, involving synthesis of formula (III) according to present invention.EFFECT: technical result is obtaining a compound of formula (III) with high output and regioselectivity, low cost and number of equivalents of reagents.10 cl, 1 tbl, 3 ex
申请公布号 RU2603261(C2) 申请公布日期 2016.11.27
申请号 RU20130148626 申请日期 2012.03.30
申请人 Sandoz AG 发明人 FELTSMANN Volfgang;SHENE Niklas
分类号 C07D498/18 主分类号 C07D498/18
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