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Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines - Communications Chemistry

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Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines - Communications Chemistry

Spirocyclic tetrahydronaphthyridines (THNs) are valuable scaffolds for drug discovery campaigns, but access to this 3D chemical space is hampered by a lack of modular and scalable synthetic methods. We hereby report an automated, continuous flow synthesis of α-alkylated and spirocyclic 1,2,3,4-tetrahydro-1,8-naphthyridines (“1,8-THNs”), in addition to their regioisomeric 1,6-THN analogues, from abundant primary amine feedstocks.

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Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines - Communications Chemistry

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Modular, automated synthesis of spirocyclic tetrahydronaphthyridines from primary alkylamines - Communications Chemistry

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