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A concise synthesis of benzodiazepines via Rh(III) catalyzed C-H activation/ 4 + 3 annulation of easily available 1-arylpyrazolidinones with allylic acetal has been developed. The allylic acetal was employed as a novel 3C synthon in this transformation. Benzodiazepines were built under mild reaction conditions with high efficiency and chemoselectivity. The high atom-economy and easily accessible substrates reveal potential application.
Hu et al. (Wed,) studied this question.