162615-12-5Relevant articles and documents
Synthetic approaches to tetrahydro-2,7- and -1,6-naphthyridines
Sierov, Dmytro,Nazarenko, Kostiantyn,Shvydenko, Kostiantyn,Shvydenko, Tetiana,Kostyuk, Aleksandr
, (2020)
Three new tetrahydronaphthyridines were prepared starting from readily available 3-bromo-picolines. The key step of the proposed strategy consists of reduction of the imine prepared by intramolecular reaction of the acyl and amine groups. The amine group was introduced via deprotonation of the methyl group in bromopicoline, its reaction with dimethylcarbonate, reduction to the corresponding alcohol and Mitsunobu reaction with phthalamide. The acyl group was placed at the bromine position via the Stille cross-coupling reaction of tributyl(1-ethoxyvinyl)stannane followed by hydrolysis. The proposed chemical sequence allowed the multigram preparation of tetrahydro-2,7- and 1,6-naphthyridines.
ISOQUINOLINES AS INHIBITORS OF HPK1
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Paragraph 0936, (2018/10/21)
Isoquinoline compounds and their use as inhibitors of HPK1 (hematopoietic kinase 1) are described. The compounds are useful in treating HPK1-dependent disorders and enhancing an immune response. Also described are methods of inhibitng HPK1, methods of treating HPK1-dependent disorders, methods for enhancing an immune response, and methods for preparing the isoquinoline compounds.
