Tetrahedron Letters p. 5939 - 5942 (1994)
Update date:2022-07-30
Topics:
Viti, Giovanni
Giannotti, Danilo
Nannicini, Rossano
Balacco, Giuseppe
Pestellini, Vittorio
A short synthesis of a cyclic constrained analogue 1 of the potent Substance P antagonist (±) CP-96345 is described. The key feature is the formation of the benzo[b]-1,5-naphthyridine system at the very last step of the synthesis through an intramolecular arylation of an amine promoted by a strong base. If the tricyclic system was synthesized first, 2-methoxy benzylation of both the nitrogen atoms occurred.
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