Reductive Alkylation of Hydrazine Derivatives with α-Picoline-Borane and Its Applications to the Syntheses of Useful Compounds Related to Active Pharmaceutical Ingredients
作者:Tsutomu Yokomatsu、Yasushi Kawase、Takehiro Yamagishi、Jun-ya Kato、Teruo Kutsuma、Tadashi Kataoka、Takeo Iwakuma
DOI:10.1055/s-0033-1340484
日期:——
ingredients of therapeutic drugs such as isocarboxazid. An efficient method for the direct reductive alkylation of hydrazine derivatives with α-picoline-borane has been developed to synthesize a variety of N-alkylhydrazine derivatives. This method provided N,N-dialkylhydrazine derivatives and N-monoalkylhydrazine derivatives upon fine-tuning of the substrates and the reagent equivalency in a one-pot manner
摘要 已经开发了一种用α-甲基吡啶-硼烷对肼衍生物进行直接还原烷基化的有效方法,以合成多种N-烷基肼衍生物。通过一锅法对底物和试剂当量进行微调,该方法提供了N,N-二烷基肼衍生物和N-单烷基肼衍生物。该方法用于合成治疗药物如异咔唑的活性药物成分。 已经开发了一种用α-甲基吡啶-硼烷对肼衍生物进行直接还原烷基化的有效方法,以合成多种N-烷基肼衍生物。通过一锅法对底物和试剂当量进行微调,该方法提供了N,N-二烷基肼衍生物和N-单烷基肼衍生物。该方法用于合成治疗药物如异咔唑的活性药物成分。