Facile Pyridine S N Ar Reactions via N-Phosphonium-Pyridinium Intermediates

Synlett. 2021 Jan;32(2):215-218. doi: 10.1055/a-1315-1279. Epub 2020 Nov 19.

Abstract

Here we report that N-phosphonium pyridinium intermediates are unusually reactive for pyridine S N Ar reactions. Specifically, forming phosphonium salts from halopyridines typically requires elevated temperatures and Lewis acid additives. The alternative activation mode described in this paper permits C-P bond formation to occur at ambient temperatures in many cases, and functions across a broad range of substrates.

Keywords: SNAr reaction; phosphonium salts; pyridines; pyridinium salts.