A General Minisci‐Type Alkylation with Organoboron Derivatives Assisted by Catechol

Abstract This manuscript describes a general strategy for the easily scale‐up alkylation of heterocycles with a wide variety of boronic acids, boronates, and trifluoroborate salts under low‐cost and simple conditions without using any transition‐metal or organo‐photocatalysts. The key additive of catechol plays an important role in this method which in‐situ activated a variety of boron‐base species to alkylboronic esters (R‐BCat) with a low oxidation potential. The transformation is distinguished by a broad scope, such as drug molecules and natural products. Furthermore, the methodology proves easily scalable under standard batch conditions, enhancing its practicality and accessibility.