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1. 发明授权

US4262013A Mevalonolactone derivatives and process for the preparation thereof 失效
标题翻译：甲酰戊内酯衍生物及其制备方法
公开(公告)号：US4262013A
公开(公告)日：1981-04-14
申请号：US63549
申请日：1979-08-03
申请人： Seiji Mistui , Akira Ogiso , Akira Indo
发明人： Seiji Mistui , Akira Ogiso , Akira Indo
IPC分类号： A61K31/365 , A61K31/366 , A61P3/06 , A61P9/10 , C07C45/72 , C07C49/223 , C07C49/255 , C07D309/30
CPC分类号： C07D309/30 , C07C45/72
摘要： 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.
摘要翻译：本发明涉及具有下式的新型甲羟戊酸内酯衍生物：其中A代表直链，亚甲基，亚乙基，三亚甲基或亚乙烯基; R1代表氢原子，脂族酰基，苯甲酰基或被羟基，低级烷氧基，脂族酰氧基或卤素取代的苯甲酰基; R2表示氢原子，卤素原子或甲基; 并且R 3，R 4和R 5相同或不同，各自表示氢原子，卤原子，具有或不具有卤素作为取代基的低级烷基，苯基或被卤素，低级烷氧基，脂族酰氧基或低级具有或不具有卤素的烷基或由式R6O-表示的基团（在式中，R6表示氢原子，脂族酰基，苯甲酰基，苯基，苯基烷基，肉桂基或苯甲酰基，苯基，其中所有芳基被羟基，卤素，低级烷氧基，脂族酰氧基或具有或不具有卤素作为取代基的低级烷基或具有或不具有卤素作为取代基的低级烷基取代的苯基烷基或肉桂基）。该化合物可用于治疗高脂血症。它们可以通过卤代 - 内酯化相应的γ，β-不饱和羧酸衍生物和任选地使得到的产物脱卤，或内酯化相应的δ-羟基 - 羧酸衍生物来制备。

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