N-烷基芳胺合成的研究进展

Progress in the synthesis of N-alkyl anilines

N-烷基芳胺是非常重要的有机原料和精细化工中间体,广泛应用于染料、塑料、医药和农药等领域。介绍了芳胺与烷基化试剂如卤代烃、羰基化合物、醇等进行的取代烷基化反应合成N-烷基芳胺的反应机理及烷基化工艺;重点阐述了以芳香硝基化合物为原料一锅法合成N-烷基芳胺的生产工艺,分别讨论了以羰基化合物、腈、醇作为烷基化试剂的优劣,认为以醇为烷基化试剂的反应条件温和、不需要添加任何配体,具有较好的应用前景。指出开发适合以醇为烷基化试剂的选择性高的催化剂是以后的研究方向。

N-alkyl anilines are widely used as synthetic intermediates for pharmaceuticals, agrochemicals,fine chemicals,bioactive compounds,and dyes chemicals.The mechanism and the research process of N-alkylation of aromatic amines with corresponding alkylating agents,such as alkyl halides,carbonyl compounds and alcohols were summarized in this paper.The one-pot synthesis of N-alkyl anilines from nitroaromatics as starting material with carbonyl compounds,nitriles and alcohols was highlighted.Recently,much attention has been paid to the use of alcohols as alkylating reagents for the N-alkylation of nitroaromatics due to the mild reaction conditions,without additional organic ligand.Therefore,the development of efficient catalyst for N-alkylation system with alcohol is still a challenging goal.