Synthesis of β‐Arylacyl/β‐Heteroarylacyl‐β‐alkylidene Malonates and Their Application in Substituted Pyridone Synthesis |
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Authors: | Manoj Balu Wagh R. Shankar K. Mini T. Krishnamohan M. V. Madhubabu Abir K. Pal Sarva Jayaprakash T. Krishna Vilas Dahanukar U. K. Syam Kumar C. H. Gill |
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Affiliation: | 1. Technology Development centre, Custom Pharmaceutical Services, Dr. Reddys Laboratories Ltd., , Miyapur, Hyderabad 500 049, India;2. Department of Chemistry, Dr. Babasaheb Ambedkar University, , Aurangabad, India |
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Abstract: | A novel approach has been developed for the synthesis of β‐arylacyl/β‐heteroarylacyl‐β‐alkylidine malonates in moderate to good yields by the reaction of Stork aryl and heteroaryl enamine with β‐chloroalkylidene malonates. The reaction involves conjugate (Michael) addition of Stork enamine on β‐chloroalkylidene malonates and elimination of chloride ion. These Michael adducts were utilized as intermediates for the synthesis of highly substituted 1,4‐dialkyl‐2‐oxo‐6‐aryl/hetreoaryl‐1,2‐dihydro‐pyridine‐3‐carboxylic acid ethyl esters via 5 + 1 ring annulation protocol. |
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