申请人:Sankyo Company Limited
公开号:US04262013A1
公开(公告)日:1981-04-14
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, 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的新型甲烷酸内酯衍生物:##STR1## 其中A表示直接连接、亚甲基、乙烯基、三亚甲基或乙烯基基团;R.sup.1表示氢原子、脂肪族酰基、苯甲酰基或羟基、较低的烷氧基、脂肪族酰氧基或卤素取代的苯甲酰基;R.sup.2表示氢原子、卤素原子或甲基基团;R.sup.3、R.sup.4和R.sup.5相同或不同,每个表示氢原子、卤素原子、具有或不具有卤素取代的较低烷基基团、苯基或卤素、较低的烷氧基、脂肪族酰氧基或具有或不具有卤素取代的较低烷基基团、苯基或苯基烷基基团,或由以下式表示的基团R.sup.6 O-(在式中,R.sup.6表示氢原子、脂肪族酰基、苯甲酰基、苯基、苯基烷基、肉桂基或苯甲酰基、苯基、苯基烷基或肉桂基,其中芳香环取代羟基、卤素、较低烷氧基、脂肪族酰氧基或具有或不具有卤素取代的较低烷基基团,或具有或不具有卤素取代的较低烷基基团)。这些化合物对治疗高脂血症有用。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选择性去卤素化所得产物,或内酯化相应的δ-羟基羧酸衍生物制备。