One‐pot, Direct Synthesis of 3‐Hydroxy‐3‐aryl‐1‐indanones and their 2‐Benzylidene Derivatives from 2‐Alkynylbenzophenones

Abstract

A rapid and efficient one‐pot strategy for the synthesis of 3‐hydroxy‐3‐aryl‐1‐indanones, directly from the corresponding 2‐alkynylbezophenones via a sequential carbonyl directed regioselective hydration followed by an intramolecular Aldol reaction has been reported. Further this strategy has also been extended for the efficient conversion of these 3‐hydroxy‐3‐aryl‐1‐indanone units into biologically important 2‐benzylidene‐3‐hydroxy‐3‐aryl‐1‐indanone derivatives, employing an intermolecular Aldol condensation reaction, both in a stepwise manner as well as one pot strategy. The process exhibits very good substrate scope and high reaction yields under mild reaction conditions.