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A Simple and Easily Implemented Method for the Regioselective Introduction of Deuterium into Azolo[1,5-a]pyrimidines
Gevorg G Danagulyan1,2, Henrik A Panosyan2, Vache K Gharibyan1
1Laboratory of Bioactive Azaheterocycles, Institute of Biomedicine and Pharmacy, Russian-Armenian University, Hovsep Emin Str. 123, Yerevan 0051, Armenia.
Abstract:
A method for the technically easy-to-implement synthesis of deuterium-labeled pyrazolo[1,5-a]pyrimidines and 1,2,4-triazolo[1,5-a]pyrimidines have been developed. The regioselectivity of such transformations has been shown. 1H NMR and mass spectrometric methods have proved the quantitative nature of such transformations and the kinetics of deuterium exchange has been studied. Spectrally, at different temperatures (+30 °C, -10 °C and -15 °C), the kinetics of the process was studied both in CD3OD and in deuterated alkali.
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