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    • 42. 发明申请
    • 6-HEPTYNOIC AND HEPTENOIC ACID COMPOUNDS
    • 6-HEPTYNOIC和HEPTENOIC酸化合物
    • WO1994006746A1
    • 1994-03-31
    • PCT/JP1993001349
    • 1993-09-21
    • NISSAN CHEMICAL INDUSTRIES LTD.SAGAMI CHEMICAL RESEARCH CENTERHIYAMA, TamejiroMINAMI, TatsuyaTAKAHASHI, KyokoMIYACHI, NobuhideOHARA, Yoshio
    • NISSAN CHEMICAL INDUSTRIES LTD.SAGAMI CHEMICAL RESEARCH CENTER
    • C07C59/42
    • C07D405/06C07C57/18C07D215/14C07D309/30Y02P20/55
    • A novel process for producing a 7-substituted-3,5-dihydroxy carboxylic acid compound useful as an HMG-CoA reductase inhibitor, and novel 6-heptynoic and heptenoic acid compounds, respectively represented by general formulae (1) and (2), useful as the starting material for the above process, wherein Z represents (3) or (4); A represents -CO- or -CHOR1- (wherein R1 represents hydrogen or a hydroxyl-protecting group) and B represents -CO- or -CHOR2- (wherein R2 represents hydrogen or a hydroxyl-protecting group), provided that R1 and R2 may be combined together to form a ring; R3 represents hydrogen, C1-C8 alkyl, aralkyl, aryl, silyl, lithium, sodium, potassium, calcium or RpRqRrNH (wherein Rp, Rq and Rr represent each independently hydrogen, C1-C8 alkyl, aralkyl or aryl); R6 represents hydrogen or a protective group for triple bonds; and L represents borane, aluminum, zirconium, magnesium or silyl each substituted by C1-C9 alkyl, alkylene, aralkyl, aryl, alkoxy, substituted phenoyx or halogen. The use of the invention compounds and process enables an efficient production of a 7-substituted-3,5-dihydroxy carboxlylic acid compound useful as an HMG-CoA reductase inhibitor.
    • 分别由通式(1)和(2)表示的用于制备可用作HMG-CoA还原酶抑制剂的7-取代-3,5-二羟基羧酸化合物和新的6-庚炔和庚烯酸化合物的新方法, 可用作上述方法的起始原料,其中Z表示(3)或(4); A表示-CO-或-CHOR1-(其中R1表示氢或羟基保护基),B表示-CO-或-CHOR2-(其中R2表示氢或羟基保护基),条件是R1和R2可以 结合在一起形成戒指; R3代表氢,C1-C8烷基,芳烷基,芳基,甲硅烷基,锂,钠,钾,钙或RpRqRrNH(其中Rp,Rq和Rr各自独立地为氢,C1-C8烷基,芳烷基或芳基)。 R6表示氢或三键保护基; L代表各自被C 1 -C 9烷基,亚烷基,芳烷基,芳基,烷氧基,取代的苯甲酸或卤素取代的硼烷,铝,锆,镁或甲硅烷基。 使用本发明化合物和方法能够有效地生产用作HMG-CoA还原酶抑制剂的7-取代-3,5-二羟基羧酸化合物。