2‐(Het)aryl‐N‐phosphorylpyrrolidines via Cyclization of Phosphorus Acid Amides: A Regioselective Approach

2020

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DOI 10.1002/slct.202003353
Data confidence 70 medium
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Abstract

Abstract A first successful synthesis of 2‐(het)aryl‐N‐phosphorylpyrrolidines is reported starting from readily available N‐(4,4‐diethoxybutyl)amides of P(V) acids. A range of phenols and hydroxyl‐substituted O‐heterocycles may be employed into the reaction furnishing N‐phosphorylated 2‐(het)arylpyrrolidines with up to 90 % yield. The developed method permits a presence of sensitive to phosphorylation hydroxy groups and provides the easy and regioselective entry to target compounds.