939052-79-6Relevant articles and documents
Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists
Milbank, Jared B.J.,Knauer, Christopher S.,Augelli-Szafran, Corinne E.,Sakkab-Tan, Annette T.,Lin, Kristin K.,Yamagata, Koji,Hoffman, Jennifer K.,Zhuang, Nian,Thomas, John,Galatsis, Paul,Wendt, John A.,Mickelson, John W.,Schwarz, Roy D.,Kinsora, Jack J.,Lotarski, Susan M.,Stakich, Korana,Gillespie, Kristen K.,Lam, Wing W.,Mutlib, Abdul E.
, p. 4415 - 4418 (2007)
Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site.
Iridium-Catalyzed Sequential Silylation and Borylation of Heteroarenes Based on Regioselective C?H Bond Activation
Murai, Masahito,Nishinaka, Naoki,Takai, Kazuhiko
supporting information, p. 5843 - 5847 (2018/04/20)
An iridium-catalyzed regioselective sequential silylation and borylation of heteroarenes was developed, which represents a rare example of unsymmetrical intermolecular C?H bond difunctionalization through the introduction of two different functionalities during a one-pot transformation. Although the substrate scope for the dehydrogenative silylation of heteroarenes has been limited mainly to electron-rich five-membered rings, the current reaction proceeds with both electron-rich and electron-deficient heteroarenes with the aid of heteroatom-directing C?H bond activation. The regioselectivity of the second borylation was controlled by both steric factors and the electronic effect of the silyl group installed in the first step. In combination with the classic cross-coupling reaction, this method provides rapid access to multisubstituted heteroarenes.
Gorlos-Phos for palladium-catalyzed borylation of aryl chlorides
Li, Pengbin,Fu, Chunling,Ma, Shengming
, p. 3604 - 3610 (2014/06/09)
Using a readily available form of the mono-phosphine ligand, Gorlos-Phos·HBF4, Pd-catalyzed borylation of aryl chlorides afforded aryl boronates in high yields. A variety of functional groups are well compatible with this palladium catalyzed borylation reaction. This journal is the Partner Organisations 2014.
