A General Three-Component Alkyl Petasis Boron-Mannich Reaction.

ABSTRACT: Aryl amines are one of the most common moieties in biologically active molecules, and approximately 37% of drug candidates contain aromatic amines. Recent advancements in medicinal chemistry, coined "escaping from flatland", have led to a greater focus on accessing highly functionalized C (sp³)-rich amines to improve the physicochemical and pharmacokinetic properties of compounds. This article presents a modular and operationally straightforward three-component alkyl Petasis boron-Mannich (APBM) reaction that utilizes ubiquitous starting materials, including amines, aldehydes, and alkyl boronates. By adaptation of this transformation to high-throughput experimentation (HTE), it offers rapid access to an array of diverse C(sp³)-rich complex

SUBMITTER: Hu C 

PROVIDER: S-EPMC11815978 | biostudies-literature | 2024 Aug

REPOSITORIES: biostudies-literature