申请人:Fujirebio Inc.
公开号:US05149834A1
公开(公告)日:1992-09-22
4-hydroxytetrahydropyran-2-one derivatives with general formula (I) are useful as cholesterol reducing agents as well as lipid reducing agents, serving as inhibitors of HMG-CoA reductase, and capable of inhibiting the biosynthesis of peroxidized lipids, and therefore effective for curing arteriosclerosis: ##STR1## wherein R.sub.1 represent hydrogen or a 2-tetrahydropyranyl group; R.sub.2 and R.sub.3 each represent hydrogen or an alkyl group having 1 to 6 carbon atoms; R.sub.4 represents hydrogen, an alkyl group having 1 to 6 carbon atoms, an alkenyl group having 2 to 6 carbon atoms, an aryl group, an aralkyl group, an acyl group, an aroyl group or a substituted sulfonyl group; A represents --CH.sub.2 CH.sub.2 --, or --CH.dbd.CH--; and n is an integer of 1 or 2, and intermediates for synthesizing the 4-hydroxytetrahydropyran-2-one derivatives are disclosed.
具有一般式(I)的4-羟基四氢吡喃-2-酮衍生物可用作降低胆固醇和脂质的药剂,作为HMG-CoA还原酶的抑制剂,能够抑制过氧化脂质的生物合成,因此对治疗动脉硬化有效:其中R.sub.1代表氢或2-四氢吡喃基团;R.sub.2和R.sub.3各代表氢或具有1至6个碳原子的烷基基团;R.sub.4代表氢,具有1至6个碳原子的烷基基团,具有2至6个碳原子的烯基基团,芳基,芳基烷基,酰基,芳基酰基或取代磺酰基;A代表--CH.sub.2 CH.sub.2--或--CH.dbd.CH--; n为1或2的整数,公开了用于合成4-羟基四氢吡喃-2-酮衍生物的中间体。