Journal
EUROPEAN JOURNAL OF ORGANIC CHEMISTRY
Volume 2017, Issue 31, Pages 4600-4608Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ejoc.201700668
Keywords
Nitrogen heterocycles; Iodine; Cyclization; Regioselectivity; Cross-coupling
Categories
Funding
- Council of Scientific and Industrial Research (CSIR), India [02(0200)/14/EMR-II]
- Central University of Rajasthan
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A highly facile single-step synthetic approach to 3-iodoquinolines has been developed for the first time from readily available 2-aminobenzophenones and terminal alkynes. The reaction involves the nucleophilic addition of terminal alkynes to 2-aminobenzophenones followed by a regioselective iodocyclization (6-endo-dig) to furnish 2,4-disubstituted 3-iodoquinolines in high yields. In general, 2,4-diaryl-substituted products were isolated without the need for column chromatography.
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