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Synthesis of Saturated 1,4-Benzodiazepines via Pd-Catalyzed Carboamination Reactions.

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journal contribution
posted on 06.05.2011 by Joshua D. Neukom, Alvin S. Aquino, John P. Wolfe
A new synthesis of 1,4-benzodiazepines and 1,4-benzodiazepin-5-ones is reported. The Pd-catalyzed coupling of N-allyl-2-aminobenzylamine derivatives with aryl bromides affords the heterocyclic products in good yield, and substrates bearing allylic methyl groups are transformed to cis-2,3-disubstituted products with >20:1 dr.