1P15: m) Design and biological evaluation of a series of thiophene-based 3-hydroxy-3-methylglutaryl coenzyme a reductase inhibitors

G. M. Coppola et al.⁴⁷ prepared a series of highly functionalized thiophene-based 3, 5-dihydroxyheptenoic acid derivatives (69) from aldehydes 64 by homologation, aldol condensation with ethyl acetoacetate dianion and stereoselective β-hydroxyketone reduction. High levels of HMG-CoA reductase inhibitory activity have been found within the series (Scheme 15).

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47. G. M. Coppola, R. E. Damon, H. Yu and R. G. Engstrom, Bioorg. Med. Chem. Lett., 1997, 7, 549.


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