申请人:Sankyo Company Limited
公开号:US04198425A1
公开(公告)日:1980-04-15
This invention concerns novel mevalonolactone derivatives having the formula ##STR1## wherein A represents a direct linkage, methylene, ethylene, trimethylene or vinylene group; R.sup.1 represents hydrogen atom, or an aliphatic acyl group, benzoyl group, or a benzoyl group substituted with hydroxy, lower alkoxy, aliphatic acyloxy or halogen; R.sup.2 represents hydrogen atom, a halogen atom or methyl group; and R.sup.3, R.sup.4 and R.sup.5 are same or different and each represents hydrogen atom, a halogen atom, a lower alkyl group with or without halogen as the substituent, phenyl group, or a phenyl group substituted with halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen, or a group represented by the formula R.sup.6 O-- (in the formula, R.sup.6 means hydrogen atom, an aliphatic acyl group, benzoyl group, phenyl group, a phenylalkyl group, cinnamyl group, or a group of benzoyl, phenyl, phenylalkyl or cinnamyl in all of which the aromatic ring is substituted with hydroxy, halogen, lower alkoxy, aliphatic acyloxy or lower alkyl with or without halogen as the substituent, or a lower alkyl group with or without halogen as the substituent). The compounds are useful for the treatment of hyperlipidemia. They may be prepared by halo-lactonizing the corresponding .gamma.,.delta.-unsaturated carboxylic acid derivatives and optionally dehalogenating the resulting product, or lactonizing the corresponding .delta.-hydroxy-carboxylic acid derivatives.
本发明涉及具有以下式子的新型甲烷基酮内酯衍生物:##STR1## 其中A代表直接连接,亚甲基,乙烯基,三亚甲基或乙烯基基团;R.sup.1代表氢原子,或脂肪族酰基,苯甲酰基,或取代羟基,较低烷氧基,脂肪族酰氧基或卤素的苯甲酰基;R.sup.2代表氢原子,卤素原子或甲基基团;R.sup.3,R.sup.4和R.sup.5相同或不同,每个代表氢原子,卤素原子,带或不带卤素的较低烷基基团,苯基,或取代卤素,较低烷氧基,脂肪族酰氧基或带或不带卤素的较低烷基的苯基,或由以下式子表示的基团R.sup.6 O-(在该式中,R.sup.6代表氢原子,脂肪族酰基,苯甲酰基,苯基,苯基烷基,肉桂酰基或苯甲酰基,苯基,苯基烷基或肉桂酰基,其中芳香环取代羟基,卤素,较低烷氧基,脂肪族酰氧基或带或不带卤素的较低烷基,或带或不带卤素的较低烷基)。这些化合物对于治疗高脂血症很有用。它们可以通过卤代内酯化相应的γ,δ-不饱和羧酸衍生物并可选地去卤生成产物,或通过内酯化相应的δ-羟基羧酸衍生物制备。