首页> 外国专利> process for the production of rechtsdrehenden enantiomers of 1 - pyridyl - 1 - (hydroxy or ethoxy) - ethyl - 4 - (o - methoxyphenyl) piperazine

process for the production of rechtsdrehenden enantiomers of 1 - pyridyl - 1 - (hydroxy or ethoxy) - ethyl - 4 - (o - methoxyphenyl) piperazine

机译:1-吡啶基-1-(羟基或乙氧基)-乙基-4-(邻甲氧基苯基)哌嗪的瑞驰缩丁烯对映体的制备方法

摘要

A process for the preparation of 1-pyridyl-alkyl-4-aryl piperazines, in the racemic form, of the formula IMAGE (I) in which: the pyridine ring is alpha-, beta-, or gamma-substituted; R=H; CnH2n+1, n being in the range from 1 to 4; R'=H, halogen, CH3, OCH3, in which process: (a) pyridine aldehyde is reacted between -5 DEG C. and 0 DEG C. with (CH3)2S=CH2; (b) the oxirane so obtained is treated with an arylpiperazine; (c) the hydroxyl derivative obtained in (b), after salification with alkaline hydrides or hydrates in a solvent medium is treated with alkylating agents, and the separation of the compounds so obtained into the respective optical antipodes.
机译:(I)的外消旋形式的1-吡啶基-烷基-4-芳基哌嗪的制备方法,其中:吡啶环被α-,β-或γ-取代; R = H; CnH2n + 1,n为1〜4; R′= H,卤素,CH3,OCH3,在此过程中:(a)吡啶醛在-5℃和0℃之间与(CH3)2S = CH2反应; (b)如此得到的环氧乙烷用芳基哌嗪处理; (c)在(b)中获得的羟基衍生物在溶剂介质中用碱金属氢化物或水合物成盐后,用烷基化剂处理,并将由此获得的化合物分离成各个旋光对映体。

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