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A HIGHLY EFFICIENT SYNTHETIC PROCESS FOR THE PREPARATION OF SIMVASTATIN AND NEW INTERMEDIATES THEREFOR

机译:一种高效的辛伐他汀的合成方法及其新的中间体

摘要

PURPOSE: A process for preparing simvastatin and intermediates used therefor are provided, thereby increasing preparation yield of simvastin and decreasing production of by-products. CONSTITUTION: A compound, is represented by the formula(1), wherein R is trialkylsilyl group represented by R1R2R3Si; and R1, R2 and R3 are the same or different, independently C1-C5 linear or branched chain alkyl. A compound is represented by the formula(2), A process for preparing simvastatin using the above compounds as intermediates comprises the steps of: preparing the compound of the formula(1) from a compound of the formula(3); preparing a compound of the formula(2) using the compound of the formula(1); and preparing simvastatin of the formula(4) using the compound of the formula(2), wherein R1R2R3Si is selected from tertiary-butyldimethylsilyl, triethylsilyl, triisopropylsilyl, phenyldimethylsilyl and diphenylmethylsilyl.
机译:用途:提供了一种制备辛伐他汀的方法及其所用的中间体,从而提高了辛伐他汀的制备产率并减少了副产物的产生。组成:一种化合物,由式(1)表示,其中R为由R1R2R3Si表示的三烷基甲硅烷基; R1,R2和R3相同或不同,独立地为C1-C5直链或支链烷基。化合物由式(2)表示。以上述化合物为中间体制备辛伐他汀的方法包括以下步骤:由式(3)的化合物制备式(1)的化合物;使用式(1)的化合物制备式(2)的化合物;使用式(2)的化合物制备式(4)的辛伐他汀,其中R 1 R 2 R 3 Si选自叔丁基二甲基甲硅烷基,三乙基甲硅烷基,三异丙基甲硅烷基,苯基二甲基甲硅烷基和二苯基甲基甲硅烷基。

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