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US5763646A Process for manufacturing simvastatin from lovastatin or mevinolinic acid 失效
从洛伐他汀或甲维林酸生产辛伐他汀的方法

Process for manufacturing simvastatin from lovastatin or mevinolinic acid
Abstract:
A process for preparing simvastatin from lovastatin or mevinolinic acid in salt form comprises treating either starting material with cyclopropyl or butyl amine, the pyranone ring thereby being opened when lovastatin is the starting material, adding a methyl group to the 2-methylbutyrate side chain, and thereafter closing the open pyranone ring to produce simvastatin. The process is performed without protecting and deprotecting the two hydroxy groups of the open pyranone ring. In a preferred embodiment, the starting material is treated with cyclopropyl amine which produces simvastatin via the novel intermediate lovastatin cyclopropyl amide.
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