5757-81-3Relevant articles and documents
A novel series of metabotropic glutamate receptor 5 negative allosteric modulators based on a 4,5,6,7-tetrahydropyrazolo[1,5-a]pyridine core
Duvey, Guillaume,Perry, Benjamin,Le Poul, Emmanuel,Poli, Sonia,Bonnet, Beatrice,Lambeng, Nathalie,Charvin, Delphine,Donovan-Rodrigues, Tansy,Haddouk, Hasnaà,Gagliardi, Stefania,Rocher, Jean-Philippe
, p. 4523 - 4527 (2013/08/23)
A series of potent non-acetylinic negative allosteric modulators of the metabotropic glutamate receptor 5 (mGlu5 NAMs) was developed starting from HTS screening hit 1. Potency was improved via iterative SAR, and physicochemical properties were optimized to deliver orally bioavailable compounds acceptable for in vivo testing. A lead molecule from the series demonstrated dose-dependent activity in the second phase of the rat formalin test from 30 mg/kg, and a preliminary PK/PD relationship was established.
Synthesis of isoquinolines via Rh(III)-catalyzed C-H activation using hydrazone as a new oxidizing directing group
Chuang, Sheng-Chieh,Gandeepan, Parthasarathy,Cheng, Chien-Hong
supporting information, p. 5750 - 5753 (2013/12/04)
An efficient and mechanistically interesting method for the synthesis of highly substituted isoquinolines by a Rh(III)-catalyzed hydrazone directed ortho C-H bond activation and annulation without an external oxidant is described. This reaction is accomplished via a C-C and C-N bond formation along with N-N bond cleavage.
Highly efficient Narasaka-Heck cyclizations mediated by P(3,5-(CF 3)2C6H3)3: Facile access to N-heterobicyclic scaffolds
Faulkner, Adele,Bower, John F.
supporting information; experimental part, p. 1675 - 1679 (2012/04/05)
N-heterobicyclic scaffolds: Highly efficient palladium-catalyzed cyclizations of oxime esters with cyclic alkenes were used as a general entry to perhydroindole and related scaffolds. The chemistry is reliant upon the use of P(3,5-(CF3)2/