Abstract
A general methodology “malonic ester amide synthesis” has been demonstrated, which uses α-substituted/unsubstituted diethyl malonates for the decarboxylative acylation of various aromatic/heteroaromatic primary/secondary amines to form one-carbon homologated amides, thus providing easy access to amides with odd/even chain lengths and an array of substituents on the alkyl/aryl part while avoiding use of acyl chlorides or peptide coupling reagents.
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GRAPHICAL ABSTRACT
ACKNOWLEDGMENTS
P. S. M. and J. P. M. thank the Council of Scientific and Industrial Research (CSIR), New Delhi, for the research fellowship. S. B. M. thanks the Department of Science and Technology (DST), New Delhi for the Ramanujan fellowship award and DST-Science and Engineering Research Council (SERC) Fast-Track project research grant. S. B. M. also thanks CSIR, New Delhi, and S. Pal, director, National Chemical Laboratory Pune, for providing the infrastructure, constant support, and encouragement.
Notes
a Single step, 120 °C, 1 h (Cs2CO3 was not necessary, self-catalyzed).
a α-Substituted DEM was purchased or prepared.[ Citation 18 , 26–30 ]
b Step 1, 12 h. Step 2, 5 h.
c Single step, 120 °C, 1 h (Cs2CO3 was not required, self-catalyzed).