阿瑞匹坦中间体3-氯甲基-1,2,4-三唑啉-5-酮的合成
아서필탄중간체3-록갑기-1,2,4-삼서람-5-동적합성
Synthesis of 3-chloromethyl-1,2,4-triazolin-5-one as Intermediate of Aprepitant
  • 万方数据
    河南科学 하남과학
    HENAN SCIENCE
    2013年 4期 436-437 ,共2页

    代本才%王兰天%霍萃萌%陈瑨%赵永德

    대본재%왕란천%곽췌맹%진진%조영덕

    阿瑞匹坦%3-氯甲基-1,2,4-三唑啉-5-酮%合成 阿瑞匹坦%3-氯甲基-1,2,4-三唑啉-5-酮%閤成
    아서필탄%3-록갑기-1,2,4-삼서람-5-동%합성
    Aprepitant%3-chloromethyl-1,2,4-triazolin-5-one%synthesis
    以水合肼、尿素为原料经缩合合成氨基脲,盐酸化后得到盐酸氨基脲,盐酸氨基脲在室温条件下与2-氯-1,1,1-三甲氧基乙烷环合得到阿瑞匹坦中间体3-氯甲基-1,2,4-三唑啉-5-酮,总产率87.0%,纯度98.5%.
    이수합정、뇨소위원료경축합합성안기뇨,염산화후득도염산안기뇨,염산안기뇨재실온조건하여2-록-1,1,1-삼갑양기을완배합득도아서필탄중간체3-록갑기-1,2,4-삼서람-5-동,총산솔87.0%,순도98.5%.
    @@@@Semicarbazide was synthesized from hydrazine hydrate and urea via condensation,and then prepared carbamylhydrazine hydrochloride by adding hydrochloric acid,followed by the cyclization with 2-chloro-1,1,1-trimethoxyethane,the authors obtained 3-chloromethyl-1,2,4-triazolin-5-one as intermediate of Aprepitant. The total yield of the target compound was 54%and the purity of the product could reached 98.5%.
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