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
1
to R
5
are as defined herein. In preferred embodiments R
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 α,β-unsaturated carboxylic acids.
本披露描述了一种操作简单的低温、催化活化
羧酸进行有机反应的方法,特别是用于与胺直接进行酰胺化反应。该方法涉及使用式(I)的邻取代芳基
硼酸,其中基团R1至R5如本文所定义。在优选实施例中,R1是卤素。芳基
硼酸催化亲核1,2-加成反应、共轭1,4-加成反应和环加成反应,包括涉及α,β-不饱和
羧酸的Diels-Alder反应。