NOVEL HMG-COA REDUCTASE INHIBITOR

Title:

NOVEL HMG-COA REDUCTASE INHIBITOR

Document Type and Number:

Japanese Patent JPH021427

Kind Code:

A

Abstract:

NEW MATERIAL: Compounds of formulas I, II (R is CH3, CH2OH, CO2H, etc.; R1 is 1-3C alkyl, 1-3C alkoxy, halogen, etc.; R2 is H at 4-5 positions, 1-3C alkyl or 2-4C alkoxy; Z is H, 1-5C alkyl, etc.) and their salts.

EXAMPLE: 6(R)-[2-8(S)-(2-Chlorobenzoyloxy)-2(S), 6-(R)-dimethyl-1,2,6,7,8,8a(R)- hexahydronaphthyl-1(S)] ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one.

USE: Hydroxymethyl glutaryl coenzyme A reductanse inhibitor useful as an antihypercholesterolemia agent.

PROCESS: 8-Acyloxy group of lovastatin is hydrolyzed, and after 4-OH of lactone being protected, 8-OH of naphthyl ring is esterified by an appropriate acyl halide to obtain a compound of formula I (R is α-arranged CH3).

Inventors:

JIYON PURUU
ARUBAATO EE DEIINA
KURARENSU ESU RUUNII

Application Number:

JP2095989A

Publication Date:

January 05, 1990

Filing Date:

February 01, 1989

Export Citation:

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Assignee:

MERCK & CO INC

International Classes:

A61K31/235; A61K31/365; A61P3/06; C07C69/76; C07C69/92; C07C239/22; C07C323/62; C07D309/30; (IPC1-7): A61K31/235; A61K31/365; C07C69/76; C07C69/92; C07C239/22; C07C323/62; C07D309/30

Attorney, Agent or Firm:

Masao Okabe (3 others)

Next Patent: PRODUCTION OF HYDROXYBENZOIC ACID ESTER