首页> 外国专利> 6(R)-(2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl)-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones, the hydroxy acid form of said pyranones, the pharmaceutically acceptable salts of said hydroxy acids, and the lower alkyl, and phenyl, dimethylamino or acetylamino substituted lower alkyl esters of said hydroxy acid, processes for preparing the same, and a pharmaceutical antihypercholesterolemic composition containing the same

6(R)-(2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen)-polyhydronaphthyl-1')-ethyl)-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones, the hydroxy acid form of said pyranones, the pharmaceutically acceptable salts of said hydroxy acids, and the lower alkyl, and phenyl, dimethylamino or acetylamino substituted lower alkyl esters of said hydroxy acid, processes for preparing the same, and a pharmaceutical antihypercholesterolemic composition containing the same

机译:6(R)-(2-(8'-酰氧基-2'-甲基-6'-甲基(或氢)-聚氢萘基-1')-乙基)-4(R)-羟基-3,4,5, 6-四氢-2H-吡喃-2-酮,所述吡喃酮的羟基酸形式,所述羟基酸的药学上可接受的盐以及所述羟基酸的低级烷基和苯基,二甲基氨基或乙酰氨基取代的低级烷基酯用于制备该药物的药物,以及包含该药物的抗高血压药的药物组合物

摘要

6(R)-(2-(8'-acyloxy-2'-methyl-6'-methyl (or hydrogen) -polyhydronaphthyl-1')-ethyl]-4(R) -hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones are prepared by acylation of the corresponding 8'-hydroxy compounds. The products are strong inhibitors of the biosynthesis of cholesterol.;The 8'-hydroxy compounds are prepared by hydrolysis of the corresponding, naturally occurring 8'-(2(S)-methylbutyryloxy) compounds with a strong base at elevated temperatures to remove the acyl group.
机译:6(R)-(2-(8'-酰氧基-2'-甲基-6'-甲基(或氢)-聚氢萘基-1')-乙基] -4(R)-羟基-3,4,5,通过酰化相应的8'-羟基化合物制备6-四氢-2H-吡喃-2-酮;这些产物是胆固醇生物合成的强抑制剂。;通过水解相应的8'-羟基化合物,天然存在的8'-(2(S)-甲基丁酰氧基)化合物,在高温下具有强碱,可去除酰基。

著录项

  • 公开/公告号EP0033538A3

    专利类型

  • 公开/公告日1982-02-24

    原文格式PDF

  • 申请/专利权人 MERCK & CO. INC.;

    申请/专利号EP19810100729

  • 申请日1981-02-02

  • 分类号C07D309/30;C07C69/30;A61K31/22;A61K31/365;C07C59/11;

  • 国家 EP

  • 入库时间 2022-08-22 13:09:11

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