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Palladium‐Catalyzed Regioselective Direct Arylation of Benzofurazans at the C‐4 Position
Author(s) -
Idris Imane,
Derridj Fazia,
Soulé JeanFrançois,
Doucet Henri
Publication year - 2017
Publication title -
advanced synthesis and catalysis
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.541
H-Index - 155
eISSN - 1615-4169
pISSN - 1615-4150
DOI - 10.1002/adsc.201700435
Subject(s) - palladium , aryl , catalysis , chemistry , bromide , phosphine , regioselectivity , derivatization , organic chemistry , potassium bromide , combinatorial chemistry , medicinal chemistry , alkyl , high performance liquid chromatography
The palladium‐catalyzed direct arylation of benzofurazans with aryl bromides to access 4‐arylbenzofurazans proceeds in moderate‐to‐high yields using phosphine‐free palladium acetate as the catalyst and potassium acetate as an inexpensive base. A wide variety of (hetero)aryl bromides, including bromopyridine and bromothiophene derivatives has been successfully employed. Palladium‐catalyzed one‐pot C‐4,C‐7‐diarylation of benzofurazan was also achieved using a larger amount of aryl bromide. Moreover, the derivatization of 4‐arylbenzofurazans into 4‐arylquinaxolines is also reported.