RAPID AND EFFICIENT BIOORTHOGONAL LIGATION REACTION AND BORON-CONTAINING HETEROCYCLES USEFUL IN CONJUNCTION THEREWITH

摘要

A reaction method comprising combining a carbonyl-substituted arylboronic acid or ester and an α-effect amine in aqueous solution at a temperature between about −5 C to 55 C, and a pH between 2 and 8 to produce an adduct. A process is also provided comprising: contacting a composition having a boron atom bonded to a sp2 hybridized carbon, the boron having at least one labile substituent, conjugated with a cis-carbonyl, with an α-effect amine, in an aqueous medium for a time sufficient to form an adduct, which may proceed to further products.

主权项

1. A process comprising:
(a) providing:
(1) a composition having a boron atom bonded to a sp2 hybridized carbon, the boron having at least one labile substituent, conjugated with a cis-carbonyl; and(2) an α-effect amine; and (b) contacting the composition with the α-effect amine, in a solvent, to spontaneously form an adduct.