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Palladium‐Catalyzed Trifluoromethylation of (Hetero)Arenes with CF 3 Br
Author(s) -
Natte Kishore,
Jagadeesh Rajenahally V.,
He Lin,
Rabeah Jabor,
Chen Jianbin,
Taeschler Christoph,
Ellinger Stefan,
Zaragoza Florencio,
Neumann Helfried,
Brückner Angelika,
Beller Matthias
Publication year - 2016
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201511131
Subject(s) - trifluoromethylation , chemoselectivity , palladium , catalysis , chemistry , combinatorial chemistry , pentoxifylline , trifluoromethyl , organic chemistry , alkyl , medicine , pharmacology
The CF 3 group is an omnipresent motif found in many pharmaceuticals, agrochemicals, catalysts, materials, and industrial chemicals. Despite well‐established trifluoromethylation methodologies, the straightforward and selective introduction of such groups into (hetero)arenes using available and less expensive sources is still a major challenge. In this regard, the selective synthesis of various trifluoromethyl‐substituted (hetero)arenes by palladium‐catalyzed C−H functionalization is herein reported. This novel methodology proceeds under comparably mild reaction conditions with good regio‐ and chemoselectivity. As examples, trifluoromethylations of biologically important molecules, such as melatonin, theophylline, caffeine, and pentoxifylline, are showcased.

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