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.
Copper-catalysed borylation of aryl chlorides
Kuehn, Laura,Huang, Mingming,Radius, Udo,Marder, Todd B.
supporting information, p. 6601 - 6606 (2019/07/16)
We report herein the first Cu-catalysed borylation of a wide range of aryl chlorides with different electronic and steric properties using a readily prepared NHC-stabilised Cu catalyst and KOtBu as the base with B2pin2 (pin = pinacolato) as the boron reagent. The aryl chlorides are converted into their corresponding arylboronic esters in good yields. The new procedure shows broad functional group tolerance, and B2neop2 (neop = neopentyl glycolato) can also be applied as the boron reagent.
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.
Iminothiadiazine Dioxide Compounds as BACE Inhibitors, Compositions and Their Use
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Paragraph 0639, (2015/11/16)
In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's disease, are also disclosed.
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.
Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists
Kulkarni, Santosh S.,Newman, Amy Hauck
, p. 2987 - 2991 (2008/02/07)
Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5.
