A straightforward concise synthesis of chiral non-racemic aliphatic α-boryl isocyanides, relay intermediates for boron-based bioactive molecules in multicomponent reactions, is presented. The short synthetic sequence comprises as key steps copper-catalysed asymmetric borylation of imines, simultaneous nitrogen formylation/boron-protecting group interconversion and the final formamide dehydration reaction.
F. Fini, A. Zanni, M. L. Introvigne, M. Stucchi, E. Caselli and F. Prati, Org. Biomol. Chem., 2021, 19, 6687 DOI: 10.1039/D1OB00616A
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