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We report a novel Wolff rearrangement/3 + 3 cycloaddition cascade for efficient synthesis of pyrimidinone derivatives from alkynyl diazoalkyl ketones and aminopyridine or aminothiazole, achieving yields up to 99% with excellent regioselectivity. The protocol demonstrates remarkable efficiency and substrate tolerance, offering potential for nucleobase modification and the development of antimicrobial agrochemicals.
Ji et al. (Wed,) studied this question.