N-叔丁基-N-取代苯甲酰肼的合成研究

采用四种不同的氨基保护法合成了九个 N 叔丁基 N (取代)苯甲酰肼,其中,氯甲酸苄酯保护法和氯甲酸苯酯保护法首次被用于该类化合物的合成,氯甲酸苄酯保护法具有反应条件温和、收率高、后处理简单及污染小等优点,适宜大规模工业生产。但是,该法的局限性是当苯环上有氯、溴或硝基等取代基时,不宜采用该法。此时,Boc保护法和氯甲酸苯酯保护法适宜作为该法的补充。

Synthesis of N-tert-Butyl-N-Substitutedbenzoylhydrazines

Nine of N-tert-butyl-N-substitutedbenzoylhydrazines were synthesized by four different processes, among them, the method of Cbz protection of amino- group enjoys a number of advantages in that the reaction is carried out under mild conditions in good yields, the experimental procedure is very simple and this method may be applicable to large-scale production. While the method can not be applied when the substituted groups on benzene ring are chloro, bromo or nitro, for the deprotection would result in the halogens on benzene ring partly losing or the nitro on the benzene reduction, and the method of Boc protection of amino- group or the method of phenyl chloroformate protection of amino- group may be applied as supplements.