申请人:FUJIREBIO Inc.
公开号:EP0617000A2
公开(公告)日:1994-09-28
A 4-fluorobiphenyl derivative of formula (I), which is useful as a cholesterol lowering agent or a lipid lowering agent because of its strong inhibitory effect on HMG-CoA reductase), and which is also useful as an intermediate for producing the above-mentioned cholesterol lowering agent or lipid lowering agent:
wherein A is a ω-oxycarbonyldihydroxybutyl group, a tetrahydropyranyl group, a ω-oxycarbonyl-3-oxobutyl group, a formyl group, or a cyano group; R¹ is a halogen atom, an alkyl group, or a group represented by R⁵O-, wherein R⁵ is a hydrogen atom, or an alkyl group; R² is a hydrogen atom, an alkyl group; R³ is a hydrogen atom, or an alkyl group; R⁵ and R² may form a five-membered ring or a six-membered ring in combination with the oxygen atoms to which R⁵ and R² are respectively bonded, and R⁵ and R³ may form a five-membered ring or a six-membered ring in combination with the oxygen atom to which R⁵ is bonded.
式(I)的 4-氟联苯衍生物,因其对 HMG-CoA 还原酶有很强的抑制作用,可用作降胆固醇剂或降血脂剂,也可用作生产上述降胆固醇剂或降血脂剂的中间体:
其中 A 是ω-氧羰基二羟基丁基、四氢吡喃基、ω-氧羰基-3-氧代丁基、甲酰基或氰基;R¹ 是卤素原子、烷基或由 R⁵O- 代表的基团,其中 R⁵ 是氢原子或烷基;R² 是氢原子、烷基;R³ 是氢原子或烷基;R⁵ 和 R² 可与分别与 R⁵ 和 R² 键合的氧原子结合形成五元环或六元环,R⁵ 和 R³ 可与与 R⁵ 键合的氧原子结合形成五元环或六元环。