Atorvastatin, an HMG??COA reductase inhibitor and efficient lipid??regulating agent. Part I. Synthesis of ring??labeled [14C6] atorvastatin

…, J Hartman, Y Huang, T Nanninga…

Index: Woo, Peter W. K.; Hartman, Jon; Huang, Yun; Nanninga, Thomas; Bauman, Kelvin; Butler, Donald E.; Rubin, John R.; Lee, Helen T.; Huang, Che C. Journal of Labelled Compounds and Radiopharmaceuticals, 1999 , vol. 42, # 2 p. 121 - 127

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Citation Number: 5

Abstract

Abstract Pyrrole-ring labeled [14 C] atorvastatin (Lipitor®, CI-981),[R-(R*, R*)]-2-(4- fluorophenyl)-β, γ-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl]-1H-[3- 14 C] pyrrole-1-heptanoic acid calcium salt (2: 1)(15), was synthesized in a 5-step synthesis from [7-14 C] benzaldehyde (5) with an overall yield of 6.9 to 9.6%. Thus, Knoevenagel condensation of 5 with isobutyryl-acetanilide (6) gave 4-methyl-3-oxo-N-phenyl-2-(phenyl ...