摘要

Phthalonitrile undergoes partial hydration in MeOH-H2O media in the presence of an equimolar amount of NaOH to afford 2-carbamimidoylbenzoic acid in good yield in one step. This and similar vic-amidino (hetero) aromatic acids also could be synthesized from corresponding 1,2-dinitriles by hydrolysis in aqueous MeOH catalyzed by an equimolar amount of NaOH of in situ generated 1,1-dimethoxy-1H-isoindol-3-amine or its counterparts. Protonation of the synthesized amidino acids, esterification, and reamination of the parent amidino benzoic acid with N-nucleophiles were performed.

  • 出版日期2017-4