首页> 外国专利> FOERFARANDE Før FRAMSTAELLNING audio ANALGETISKT VERKANDE RACE MISKA the OR DIASTEREOMERA OCH optically active 2-TETRAHYDROFURFURYL- (1R / S, 5R / S, 9R / S) -2'-hydroxy-5,9-dimethyl-6,7-OCH BENSOMORFANER deras SYRAADDITIONSSALTER

FOERFARANDE Før FRAMSTAELLNING audio ANALGETISKT VERKANDE RACE MISKA the OR DIASTEREOMERA OCH optically active 2-TETRAHYDROFURFURYL- (1R / S, 5R / S, 9R / S) -2'-hydroxy-5,9-dimethyl-6,7-OCH BENSOMORFANER deras SYRAADDITIONSSALTER

机译:程序制备音频麻醉作用MISKA或非对映体和光学活性2-四氢呋喃基-(1R / S,5R / S,9R / S)-2'-羟基-5,9-二甲基-6,7-和苯甲酸萨尔特

摘要

Novel 2-tetrahydrofurfuryl-6-7-benzomorphans of the accompanying formula I, in which R1 denotes methyl, ethyl or propyl; R2 denotes hydrogen, methyl or ethyl; R3 denotes hydrogen or methyl; and R4 denotes hydrogen, alkyl having 1 to 4 carbon atoms or acyl having 2 to 5 carbon atoms, are prepared by introducing the tetrahydrofurfuryl radical into appropriately substituted norbenzomorphans by the methods of N-alkylation. The resulting bases of the formula I can then be converted into their acid addition salts. The compounds of the formula I and their acid addition salts are distinguished by a therapeutically utilisable action on the central nervous system. Particularly to be emphasised is their analgesic action, which frequently exceeds that of morphine, without exhibiting the undesired side effects of morphine, e.g. the addictive action. IMAGE
机译:伴随式I的新型2-四氢糠基-6-7-苯并吗啉,其中R 1表示甲基,乙基或丙基; R 2表示氢,甲基或乙基; R 3表示氢或甲基; R 4表示氢,具有1至4个碳原子的烷基或具有2至5个碳原子的酰基,是通过N-烷基化方法将四氢糠基引入适当取代的去甲苯并吗啉中而制备的。然后可以将所得的式I的碱转化为其酸加成盐。式I化合物及其酸加成盐的特征在于对中枢神经系统具有治疗上可利用的作用。特别要强调的是它们的镇痛作用,通常超过吗啡的镇痛作用,而不会表现出吗啡的不良副作用,例如吗啡。上瘾的行为。 <图像>

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