Pyrrole-Aminopyrimidine Ensembles: Cycloaddition of Guanidine to Acylethynylpyrroles

吡咯-氨基嘧啶复合物:胍与乙酰乙炔基吡咯的环加成反应

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作者:Olga V Petrova, Arsalan B Budaev, Elena F Sagitova, Igor A Ushakov, Lyubov N Sobenina, Andrey V Ivanov, Boris A Trofimov

Abstract

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.

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