Sython, B.v.

Theororus Hendricus Peters

Frantisek Picha

Frans Van Dalen

Gertruda Antonetta Van Helvoirt

Jacohus Maria Lemmens

A process for the production of simvastatin and its analogues that is efficient, economical and convenient involves the use of hydroxyl protected intermediates of formula (III) or (VII). These intermediates allow for direct alkylation of the butyrate side chain followed by deprotection and reformation of the lactone ring. R.sup.1 is hydrogen or methyl; R.sup.2 represents a straight or branched chain alkyl group having 1 to 8 carbon atoms, a cycloalkyl group having 3 to 7 carbon atoms, or an aralkyl group having 1 to 6 carbon atoms in the alkyl chain; R.sup.3 and R.sup.4 each independently represent an alkyl group, an ether group, a thioether group, an aryl group, an aralkyl group, an alkenyl group, a cyclic ether group, or a cyclic thioether group; and R.sup.5 and R.sup.6 each independently represent hydrogen, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, or an ether group.

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Arnhem, Netherlands

Theororus Hendricus Peters