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Substituted aminopyrazoles (5a-d) were synthesized and reacted with bidentate electrophiles to afford pyrazolo[1,5-a]pyrimidines. The regioorientation of reagents has been determined by (N, H) HMBC measurements as well as an X-ray crystal structure determination.

2H-Pyrazol-3-ylamines as precursors for the synthesis of polyfunctionally substituted pyrazolo[1,5-a]pyrimidines