AI Article Synopsis
- * Recent advancements, known as "escaping from flatland," focus on creating more complex C()-rich amines to enhance drug properties.
- * The article describes a simple three-component reaction (APBM) using common starting materials, optimized for high-throughput experimentation to quickly produce diverse amines suitable for drug discovery.
Article 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 ()-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()-rich complex amines, amenable for rapid identification of drug candidates.
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| http://dx.doi.org/10.1021/jacs.4c05940 | DOI Listing |
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