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Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

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.

SUBMITTER: Rouquet G 

PROVIDER: S-EPMC4360148 | biostudies-literature | 2015 Mar

REPOSITORIES: biostudies-literature

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Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists.

Rouquet Guy G   Moore Dianna E DE   Spain Malcolm M   Allwood Daniel M DM   Battilocchio Claudio C   Blakemore David C DC   Fish Paul V PV   Jenkinson Stephen S   Jessiman Alan S AS   Ley Steven V SV   McMurray Gordon G   Storer R Ian RI  

ACS medicinal chemistry letters 20150120 3

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  ...[more]

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