Synthesis of oxazolo[4,5-c ]quinoline TRPV1 antagonists

Journal of Organic Chemistry

Volumn 75, Issue 24, 2010, Pages 8713-8715

  Voight, Eric A ^a   Daanen, Jerome F ^a   Kort, Michael E ^a  

^a ABBOTT LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

EFFICIENT SYNTHESIS; ION CHANNEL; SELECTIVE LIGANDS; SYNTHETIC ROUTES;

THIOUREAS; UREA;

CYCLIZATION;

8 (7 (TRIFLUOROMETHYL)OXAZOLO[4,5 C]QUINOLIN 2 YLAMINO)1,2,3,4 TETRAHYDRONAPHTHALEN 2 OL HYDROCHLORIDE HYDRATE; UNCLASSIFIED DRUG; VANILLOID RECEPTOR 1 ANTAGONIST;

ARTICLE; CHIRALITY; CYCLIZATION; ENANTIOMER; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HYDROGENATION; ONE POT SYNTHESIS;

CAPSAICIN; CRYSTALLOGRAPHY, X-RAY; HETEROCYCLIC COMPOUNDS; MAGNETIC RESONANCE SPECTROSCOPY; MOLECULAR STRUCTURE; OXAZOLES; QUINOLINES; STRUCTURE-ACTIVITY RELATIONSHIP; THIOUREA; TRPV CATION CHANNELS;

EID: 78650350318     PISSN: 00223263     EISSN: 15206904     Source Type: Journal    
DOI: 10.1021/jo101938b     Document Type: Article

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19. For in vitro assay conditions, see ref 6.
20. With the exception of compound 26, elemental analyses of final products were consistent with HCl salts containing 0.4-1.3 equiv water. Yields were calculated assuming HCl salt monohydrates (except for compound 26).