首页> 外国专利> Alpha - (adamant - (1 ') - oxy) - butyric and alpha - (adamant - (1') - oxy) - beta - methyl - butyric and method for their preparation

Alpha - (adamant - (1 ') - oxy) - butyric and alpha - (adamant - (1') - oxy) - beta - methyl - butyric and method for their preparation

机译:α-(金刚烷-(1')-氧基)-丁酸和α-(金刚烷-(1')-氧基)-β-甲基-丁酸及其制备方法

摘要

The invention comprises compounds of the general formula FORM:1028237/C2/1 wherein R1 is hydrogen, an alkyl radical of at most 5 carbon atoms or a phenyl, p-chlorophenyl or 3,4-methylenedioxyphenyl radical, R2 is hydrogen or an alkyl radical containing 1-4 carbon atoms or R2 may be bound to an alkyl radical R1 to form an alkylene radical having 2-7 chain members and 2-9 carbon atoms, and R3 represents an alkyl radical of 1-5 carbon atoms, a hydrogen atom, a monovalent cation or the normal equivalent of a polyvalent cation, and the preparation thereof either by reacting a reactive ester of 1-adamantanol with a compound of the general formula FORM:1028237/C2/2 wherein R3 is an alkyl radical and wherein R1 and R2 have the meanings given above, or a metal derivative thereof, and, if desired, hydrolysing the a -(adamant-1-yloxy)-carboxylic acid alkyl ester obtained to the free acid or to a salt, and, if desired, converting the free acid or salt into another salt with an organic or inorganic base, and, if desired, resolving a racemic acid into its antipodes, or by reacting a reactive ester of a hydroxyl compound of the last general formula above, wherein R1, R2 and R3 have the meanings given in the first general formula above, with a reactive salt of 1-adamantanol, e.g. its alkali metal salts which may be formed in situ, preferably in the absence of air. Pharmaceutical preparations having choleretic and fungistatic activity comprising a compound of the first general formula above and an inert diluent.
机译:本发明包含通式的化合物,其中R 1是氢,至多5个碳原子的烷基或苯基,对氯苯基或3,4-亚甲基二氧苯基,R 2是氢或-。含有1-4个碳原子的烷基或R 2可以与烷基R 1结合形成具有2-7个链成员和2-9个碳原子的亚烷基,并且R 3代表1-5个碳原子的烷基。氢原子,一价阳离子或多价阳离子的正当量,及其制备方法是使1-金刚烷醇的反应性酯与通式的化合物反应,其中R3为且其中R 1和R 2具有上述含义的烷基,或其金属衍生物,并且如果需要,将获得的α-(金刚烷-1-基氧基)-羧酸烷基酯水解成游离酸或成盐,并根据需要将游离酸或盐与有机或无机盐转化为另一种盐碱,并且,如果需要,将消旋酸拆分为其对映体,或通过使上述最后一个通式的羟基化合物的反应性酯反应,其中R1,R2和R3具有以上第一个通式中给出的含义,用1-金刚烷醇的活性盐,例如其碱金属盐可以原位形成,最好在没有空气的情况下形成。具有胆汁和真菌活性的药物制剂,其包含上述第一通式的化合物和惰性稀释剂。

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