A.E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch, Russian Academy of Sciences, 1 Favorsky Street, 664033 Irkutsk, Russia.
Molecules. 2021 Mar 17;26(6):1692. doi: 10.3390/molecules26061692.
An efficient method for the synthesis of pharmaceutically prospective pyrrole-aminopyrimidine ensembles (in up to 91% yield) by the cyclocondensation of easily available acylethynylpyrroles with guanidine nitrate has been developed. The reaction proceeds under heating (110-115 °C, 4 h) in the KOH/DMSO system. In the case of 2-benzoylethynylpyrrole, the unexpected addition of the formed pyrrole-aminopyrimidine as N- (NH moiety of the pyrrole ring) and C- (CH of aminopyrimidine) nucleophiles to the triple bond is observed.
开发了一种通过易得的酰基乙炔基吡咯与硝酸胍的环缩合反应高效合成具有药用前景的吡咯-氨基嘧啶混合物（产率高达 91%）的方法。该反应在 KOH/DMSO 体系中加热（110-115°C，4 小时）进行。在 2-苯甲酰基乙炔基吡咯的情况下，观察到形成的吡咯-氨基嘧啶作为 N-（吡咯环的 NH 部分）和 C-（氨基嘧啶的 CH）亲核试剂出乎意料地添加到三键中。
