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Cover Picture: Synthesis of 4‐Aryl‐2‐Quinolones via Copper‐Catalyzed Hydroarylation of ( o ‐Aminophenyl)propiolates with Arylboronates (Adv. Synth. Catal. 2/2016)
Author(s) -
Murayama Tsukasa,
Shibuya Masatoshi,
Yamamoto Yoshihiko
Publication year - 2016
Publication title -
advanced synthesis and catalysis
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 1.541
H-Index - 155
eISSN - 1615-4169
pISSN - 1615-4150
DOI - 10.1002/adsc.201501022
Subject(s) - chemistry , aryl , methanol , catalysis , carboxylation , medicinal chemistry , combinatorial chemistry , copper , organic chemistry , alkyl
The front cover image , provided by Yoshihiko Yamamoto, illustrates an efficient modular synthesis of 4‐aryl‐2(1 H )‐quinolones via one‐pot hydroarylation/cyclization. The hydroarylation of orthogonally protected ( o ‐aminophenyl)propiolates with arylboronic acid neopentyl glycol esters under mild conditions using Cu(OAc) 2 as a catalyst in methanol and the subsequent acidic removal of a Boc group afforded the 4‐aryl‐2‐quinolones. The ( o ‐aminophenyl)propiolate substrates were prepared by desilylative carboxylation of the corresponding silylalkynes using carbon dioxide as a ubiquitous C 1 source. Details can be found in the communication on pages 166–171 (T. Murayama, M. Shibuya, Y. Yamamoto, Adv. Synth. Catal. 2016 , 358 , 166–171; DOI: 10.1002/adsc.201500837 ).