Tsuruoka, Ryoji; Yoshikawa, Naoki; Konishi, Takahiro; Yamano, Mitsuhisa published the artcile< Asymmetric Synthesis of a 5,6,7,8-Tetrahydro-1,6-naphthyridine Scaffold Leading to Potent Retinoid-Related Orphan Receptor γt Inverse Agonist TAK-828F>, SDS of cas: 777931-67-6, the main research area is enantioselective synthesis TAK 828F; Heck vinylation chloropyridine ethylene; naphthyridine synthesis vinylacylpyridine ammonia; ruthenium catalyzed enantioselective transfer hydrogenation; retinoid related orphan receptor gamma t inverse agonist synthesis.
An asym. synthesis of the tetrahydronaphthyridine scaffold of TAK-828F as a RORγt inverse agonist has been developed. The synthesis features a newly discovered atom-economical protocol for Heck-type vinylation of chloropyridine using ethylene gas, an unprecedented formation of dihydronaphthyridine directly from 2-vinyl-3-acylpyridine mediated by ammonia, and a ruthenium-catalyzed enantioselective transfer hydrogenation as key steps. This represents the first example of the enantioselective synthesis of a 5,6,7,8-tetrahydro-1,6-naphthyridine compound The new synthesis is also free of chromatog. or distillation purification processes and therefore qualifies for extension to large-scale manufacture
Journal of Organic Chemistry published new progress about Arylation. 777931-67-6 belongs to class pyridine-derivatives, and the molecular formula is C6H5BrClNO, SDS of cas: 777931-67-6.