Synthesis of saturated 1,4-benzodiazepines via Pd-catalyzed carboamination reactions |
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| Authors: | Neukom Joshua D Aquino Alvin S Wolfe John P |
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| Institution: | Department of Chemistry, University of Michigan, 930 North University Avenue, Ann Arbor, Michigan 48109-1055, United States. |
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| Abstract: | 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. |
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