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  • Title: Ultrasonic-promoted three-component synthesis of some biologically active 1,2,5,6-tetrahydropyrimidines.
    Author: Muravyova EA, Desenko SM, Musatov VI, Knyazeva IV, Shishkina SV, Shishkin OV, Chebanov VA.
    Journal: J Comb Chem; 2007; 9(5):797-803. PubMed ID: 17665962.
    Abstract:
    Multicomponent reactions and organic synthesis with ultrasonic activation have been used as key methods for the synthesis of tetrahydropyrimidine derivatives. The three-component condensation of 1,3-diarylprop-2-en-1-one with ammonia and aldehydes/acetone or N-substituted gamma-pyridones under ultrasonic irradiation was developed as a rapid and efficient solution-phase method for the high-yielding preparation of 2-aryl(hetaryl)-4,6-diaryl-1,2,5,6-tetrahydropyrimidines and 2,4-diaryl-1,5,9-triazaspiro[5.5]undec-1-enes. The described synthetic protocol provides rapid access to novel and diversely substituted tetrahydropyrimidines libraries. The simple, primary biological screening showed 98% of inhibitory activity against Mycobacterium tuberculosis for one of tetrahydropyrimidines synthesized.
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