Copper-Catalyzed Enantioselective Synthesis of β-Boron β-Amino Esters,Organic Letters

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Copper-Catalyzed Enantioselective Synthesis of β-Boron β-Amino Esters
Organic Letters ( IF 4.9 ) Pub Date : 2017-11-13 00:00:00 , DOI: 10.1021/acs.orglett.7b02784
Aurora López , Timothy B. Clark ₁ , Alejandro Parra , Mariola Tortosa

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In this report, the enantioselective, copper-catalyzed borylation of β-amidoacrylates is disclosed. A broad variety of biologically important α-aminoboronates has been prepared with consistently high levels of enantiocontrol using an inexpensive copper catalyst and a commercially available chiral ligand. The method can be applied to the synthesis of novel boron-containing dipeptides and hemiboronates.

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