α-Amidoboronate esters by amide-directed alkane CH borylation

Add time:09/10/2019    Source:sciencedirect.com

α-Amidoboronic acids have received significant attention in recent years following the development of Bortezomib as an FDA-approved treatment of multiple myeloma and mantle cell lymphoma. More versatile methods to access α-amidoboronic acids continue to be developed. A direct method to access the precursors, α-amidoboronate esters, by iridium-catalyzed CH borylation of amides was developed using a readily available ligand/catalyst combination. Although the scope is limited, good yields of α-amidoboronate esters are achieved in high selectivity. Conversion of the boronate esters to the corresponding α-amidoboronic acids was also demonstrated.

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