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    • 6. 发明公开
    • 사이클로알킬 피롤 및 아졸을 가지는 피페라진 유도체 및그의 염, 및 이를 포함하는 약학 조성물
    • 具有环丙基吡咯烷酮及其盐及其盐的哌嗪衍生物及包含其的药物组合物
    • KR1020090090457A
    • 2009-08-26
    • KR1020080015671
    • 2008-02-21
    • 한국화학연구원
    • 최일영임희종이규철박우규공재양
    • C07D401/08A61K31/497
    • A piperazine derivative is provided to treat schizophrenia by antagonism to dopamine D4 receptor. A piperazine derivative is denoted by the chemical formula 1. In the chemical formula 1, R1 is structural formula a, b, c, d, e, or f, and X is hydrogen, halogen, C1-6 alkyl, C1-6 alkoxy or cyano. A method for producing the piperazine derivative of the chemical formulal Ia: a step of reacting hydrazine in substituted acetone phenone to generate hydrazone and reacting ammonium acetate to produce pyrrole ring of the chemical formula III; a step of reacting with cycloalkane under the presence of catalyst to produce a cycloalkine pyrrole; and a step of reacting reductive amination with substituted or non-substituted piperazine to produce a compound of the chemical formula Ia.
    • 提供哌嗪衍生物通过拮抗多巴胺D4受体来治疗精神分裂症。 哌嗪衍生物由化学式1表示。在化学式1中,R 1为结构式a,b,c,d,e或f,X为氢,卤素,C 1-6烷基,C 1-6烷氧基 或氰基。 制备化学式Ia的哌嗪衍生物的方法:使肼在取代的丙酮苯酮中反应生成腙并使乙酸铵反应生成化学式III的吡咯环的步骤; 在催化剂存在下与环烷烃反应生成环烷基吡咯的步骤; 以及使还原胺化与取代或未取代的哌嗪反应以产生化学式Ia的化合物的步骤。