申请人:Merck Patent Gesellschaft mit beschrankter Haftung
公开号:US04072754A1
公开(公告)日:1978-02-07
Hydratropic acid derivatives of the formula ##STR1## wherein R.sub.1 is H, alkyl of 1-4 carbon atoms, 2-acetamidoethyl, 1-methyl-4-piperidyl, or 2,3-dihydroxypropyl, and R.sub.2 is Hal, phenyl, 4-Hal-phenyl, 4-Hal-phenoxy, 4-Hal-phenoxymethyl, 1,2,3,4-tetrahydro-1-naphthyl, 1-pyrryl, piperidino, isoindolino, 1,2,3,4-tetrahydroquinolino, 1,2,3,4-tetrahydro-4-quinolyl or 1-methyl-1,2,3,4-tetrahydro-4-quinolyl, Hal being F, Cl, or Br, and the physiologically acceptable salts thereof, which possess cholesterol and triglyceride serum-level-lowering activity, can be prepared by reacting a phenol of the formula ##STR2## with a compound of the formula X--C(CH.sub.3)(C.sub. 6 H.sub.5)--COOR.sub.1 wherein X represents Cl, Br, I, OH, or esterified OH.
公式为##STR1##的羟基环戊酸衍生物,其中R.sub.1为H,1-4个碳原子的烷基,2-乙酰胺乙基,1-甲基-4-哌啶基,或2,3-二羟基丙基;R.sub.2为卤素,苯基,4-卤苯基,4-卤苯氧基,4-卤苯氧甲基,1,2,3,4-四氢-1-萘基,1-吡啶基,哌啶基,异吲哚基,1,2,3,4-四氢喹啉基,1,2,3,4-四氢-4-喹啉基或1-甲基-1,2,3,4-四氢-4-喹啉基,卤素为F,Cl或Br,以及其生理学上可接受的盐,具有降低胆固醇和甘油三酯血清水平的活性,可以通过将##STR2##的酚与公式X--C(CH.sub.3)(C.sub. 6 H.sub.5)--COOR.sub.1的化合物反应来制备。