Patent Number: 8,822,720

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

Abstract: 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 R.sup.1 to R.sup.5 are as defined herein. In preferred embodiments R.sup.1 is halogen. The arylboromc acids catalyze nucleophilic 1,2-addition reactions, conjugate 1,4-addition reactions, and cycloaddition reactions, including Diels-Alder reactions involving .alpha.,.beta.-unsaturated carboxylic acids. ##STR00001##

Inventors: Hall; Dennis (Edmonton, CA), Marion; Olivier (St. Redempteur, CA), Al-Zoubi; Raed (Edmonton, CA)

Assignee: The Governors of the University of Alberta

International Classification: C07F 5/02 (20060101)

Expiration Date: 9/02/12018