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Title:
6-(((SUBSTITUTED) PYRIDINE-3-YL)ALKYL AND ALKENYL)-TETRAHYDRO-4-HYDROXYPYRANE-2-ONE INHIBITOR OF CHOLESTEROL BIOSYNTHESIS
Document Type and Number:
Japanese Patent JPH01121266
Kind Code:
A
Abstract:

NEW MATERIAL: A compd. expressed by formula I and II (X is CH2CH2 or CH=CH; R1 and R4 are alkyl, CF3 cyclopropyl, (substd.) phenyl, 2-pyridyl, 2-pyrimidinyl, CH2OH, etc., and R1 is moreover CH2OH or S(O)nR ((n) is 0-2; R is alkyl, phenyl, etc.; R2 is H, alkyl, CF3, cyclopropyl, (substd.) phenyl, etc.; R3 is H, alkyl, CN, CH2NH2, NO2, etc.), and its N-oxide.

EXAMPLE: Trans-tetrahydro-4-hydroxy-6-[2-(2-methyl-4-phenyl-3-pyridinyl)ethyl]-2 H-pyrane-2-one.

USE: A strong inhibitor of cholesterol biosynthesis.

PROCESS: The compd. expressed by formula I is obtained by allowing the compd. expressed by formula III to react with an alkali metal salt of a dianion of methylacetoacetate, then reducing an obtained compd. expressed by formula IV to obtain an ester compd. expressed by formula V, then hydrolyzing and cyclizing the ester.


Inventors:
AREGUZANDAA UIRUHERUMU CHIYUCH
MAAKU UOORESU KURESUUERU
BURUUSU DEIBITSUDO ROSU
DORAGO ROBAATO SURISUKOBITSUKU
Application Number:
JP22259388A
Publication Date:
May 12, 1989
Filing Date:
September 07, 1988
Export Citation:
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Assignee:
WARNER LAMBERT CO
International Classes:
A61K31/4418; A61K31/443; A61P3/06; C07D213/30; C07D213/55; C07D213/61; C07D213/62; C07D213/64; C07D213/65; C07D213/71; C07D213/72; C07D213/74; C07D213/75; C07D213/79; C07D213/80; A61K31/44; C07D213/82; C07D213/84; C07D213/85; C07D213/89; C07D405/06; C07D405/14; (IPC1-7): A61K31/44; C07D213/30; C07D213/55; C07D213/61; C07D213/62; C07D213/64; C07D213/71; C07D213/72; C07D213/74; C07D213/75; C07D213/79; C07D213/84; C07D213/89; C07D405/06; C07D405/14
Attorney, Agent or Firm:
Chika Takagi (2 outside)