Rouquet, G;
Moore, DE;
Spain, M;
Allwood, DM;
Battilocchio, C;
Blakemore, DC;
Fish, PV;
... Storer, RI; + view all
(2015)
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.
ACS Medicinal Chemistry Letters
, 6
(3)
pp. 329-333.
10.1021/ml500507v.
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Abstract
A series of pyrido[3,4-d]azepines that are potent and selective 5-HT2C receptor agonists is disclosed. Compound 7 (PF-04781340) is identified as a suitable lead owing to good 5-HT2C potency, selectivity over 5-HT2B agonism, and in vitro ADME properties commensurate with an orally available and CNS penetrant profile. The synthesis of a novel bicyclic tetrasubstituted pyridine core template is outlined, including rationale to account for the unexpected formation of aminopyridine 13 resulting from an ammonia cascade cyclization.
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