Suzuki-Miyaura cross-coupling of unprotected ortho -bromoanilines with benzyl, alkyl, aryl, alkenyl and heteroaromatic boronic esters.

A Suzuki-Miyaura cross-coupling reaction was developed on unprotected ortho -bromoanilines. This operationally simple reaction was developed for the diversification of glucocorticoid receptor modulators (GRMs), showed compatibility to various boronic esters featuring unique functionalities, and was demonstrated on a gram scale.