Enantioselective synthesis of the optical isomers of broad-spectrum orally active antifungal azoles, Sch 42538 and Sch 45012

Bioorganic & Medicinal Chemistry Letters
1994.0

Abstract

Sharpless-Katsuki asymmetric epoxidation of 1 provided the (R)-(+)- and (S)-(-) epoxy alcohols 2R and 2S as key intermediates towards all six stereoisomers of the title compounds. Sch 50001 and Sch 50002 (the "eutomers" of Sch 45012) are novel antifungals which display greatly improved oral activity over itraconazole and saperconazole.

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