Journal
JOURNAL OF ORGANIC CHEMISTRY
Volume 86, Issue 7, Pages 5345-5353Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.0c02929
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Funding
- National Natural Science Foundation of China [21672177, 21931010]
- National Key R&D Program of China [2017YFA0207302]
- Program for Changjiang Scholars and Innovative Research Team in University of the Ministry of Education, China
- Natural Science Foundation of Fujian Province of China [2020J01024]
- NFFTBS [J1310024]
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A facile method for the preparation of 2,3-dialkylsubstituted quinazolinones from readily available N-arylamides and commercial isocyanates was developed, which involves the activation of the secondary amide with Tf2O/2-Br-Pyr, sequential addition of isocyanate, and cyclization. The mild reaction is general for a wide range of substrates and can be run on a gram scale.
A facile method for the preparation of 2,3-dialkylsubstituted quinazolinones from readily available N-arylamides and commercial isocyanates was developed. This one-pot procedure involves the chemoselective activation of the secondary amide with Tf2O/2-Br-Pyr, the sequential addition of isocyanate, and cyclization. The mild reaction is general for a wide range of substrates and can be run on a gram scale.
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