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US 4,282,155 AGranted
Antihypercholesterolemic compounds
AssigneeMerck & Co., Inc.
InventorsRobert L. Smith, Ta-jyh Lee
Life of this patent
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Abstract
6(R)-[2-(8'-Etherified-hydroxy-2',6'-dimethylpolyhydronaphthyl-1')-ethyl]-4 (R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones are prepared from the corresponding 8'-acyloxy compounds, some of which are naturally occurring, by protection of the 4(R)-hydroxyl and the 2-keto group, followed by reductive removal of the 8'-acyloxy group, etherification of the resulting 8'-hydroxyl and removal of the protecting groups. The products inhibit the biosynthesis of cholesterol.
Claims6
A compound of the structure:
- ##STR13## in which R is:
- C.sub.1-18 alkyl, straight or branched chain,
- C.sub.4-10 cycloalkyl,
- C.sub.2-10 alkenyl,
- C.sub.5-10 cycloalkenyl,
- C.sub.2-10 alkynyl,
- phenyl C.sub.1-3 alkyl,
- substituted phenyl C.sub.1-3 alkyl in which the substituent is halogen, CF.sub.3 or CN, and
- C.sub.1-10 alkyl having one or more --O--, --S--, or ##STR14## in the chain, in which the dotted lines at X,Y and Z represent possible double bonds, said double bonds, when any are present, being either X and Z in combination or X, Y or Z alone, and the corresponding hydroxy acids of the formula:
- ##STR15## and the pharmaceutically acceptable salts, the loweralkyl esters and the phenyl, dimethylamino and acetylamino substituted loweralkyl esters of said hydroxy acids.
7 more elements
Dependencies are inferred from the claim text.