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Microwave‐Assisted Tandem Kornblum Oxidation and Biginelli Reaction for the Synthesis of Dihydropyrimidones
Author(s) -
Malik Asif A.,
Dangroo Nisar A.,
Ara Tabassum
Publication year - 2020
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202002864
Subject(s) - tandem , biginelli reaction , catalysis , chemistry , halide , urea , combinatorial chemistry , aqueous solution , microwave , organic synthesis , microwave irradiation , organic chemistry , materials science , computer science , telecommunications , composite material
A simple and straightforward approach for the synthesis of dihydropyrimidones via sequential Kornblum oxidation/Biginelli reaction has been developed. The protocol involves an in situ oxidation of benzyl halides which serve as a carbonyl equivalents followed by cyclocondensation with (thio) urea and ethylacetoacetate to furnish dihydropyrimidones under catalyst and base free conditions in a one‐pot tandem manner under microwave irradiation. Further, the product purification using aqueous recrystallization avoids large quantities of volatile and a toxic organic solvent usually required for work‐up and very less time required for this process makes the method environmental‐ and nature‐friendly.