Sajiki Hironao, Ikawa Takashi, Hirota Kosaku
Laboratory of Medicinal Chemistry, Gifu Pharmaceutical University, Mitahora-higashi, Gifu 502-8585, Japan.
Org Lett. 2004 Dec 23;6(26):4977-80. doi: 10.1021/ol047871o.
[reaction: see text] A selective and catalytic mono-N-alkylation method of both aromatic and aliphatic amines using nitriles as an alkylating agent with Pd/C or Rh/C as a catalyst is described. This method is particularly attractive to provide an environmentally benign and applicable alkylation method of amines without using toxic and corrosive alkylating agents such as alkyl halides and carbonyl compounds.
[反应:见正文] 描述了一种以腈类为烷基化剂、Pd/C或Rh/C为催化剂,对芳香胺和脂肪胺进行选择性催化单N-烷基化的方法。该方法特别吸引人之处在于,它提供了一种环境友好且适用的胺烷基化方法,无需使用卤代烃和羰基化合物等有毒腐蚀性烷基化剂。