Method for the organocatalytic activation of carboxylic acids for chemical, reactions using orthosubstituted arylboronic acids

摘要

The present disclosure describes operationally simple methods for the low temperature, catalytic activation of carboxylic acids for organic reactions, in particular for direct amidation reactions with amines. The methods involve the use of orthosubstituted arylboromc acids of the formula (I), wherein the groups R1 to R5 are as defined herein. In preferred embodiments R1 is halogen. The arylboromc acids catalyze nucleophilic 1,2-addition reactions, conjugate 1,4-addition reactions, and cycloaddition reactions, including Diels-Alder reactions involving α,β-unsaturated carboxylic acids.;

主权项

1. A compound of the formula II: wherein: R6 is selected from H and C1-4alkyl; and R7, R8 and R9 are independently selected from H, C1-4alkyl and OC1-4alkyl and one or two of R7, R8 and R9 is H.