Atorvastatin, an HMG??COA reductase inhibitor and effective lipid??regulating agent. Part II. Synthesis of side??chain??labeled [14C] atorvastatin

HT Lee, PWK Woo

文献索引：Lee, Helen T.; Woo, Peter W. K. Journal of Labelled Compounds and Radiopharmaceuticals, 1999 , vol. 42, # 2 p. 129 - 133

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被引用次数: 7

摘要

Abstract [14 C] Atorvastatin was synthesized in a ten-step sequence with an overall yield of 5.7%. The label was introduced as sodium [1-14 C] acetate, which was converted via the acid chloride to the (S)-2-hydroxy-1, 2, 2-triphenylethyl ester 4. Chiral condensation of 4 with aldehyde 5 gave the chiral ester intermediate 6 with a yield of about 70%. Following transesterification of 6 to a methyl ester and condensation with tert-butyl lithioacetate to ...