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2005
Fused pyridine derivatives
R 0450
Synthesis of 2-Amino-3-hydroxy-4-substituted Pyridines via Regioselective Metaof 3-(1-Ethylpropyl)[1,3]oxazolo[4,5-b]pyridin-2(3H)-one and Application
26- 088 lation
to Corticotropin Releasing Factor1 Receptor Ligands. — The regioselective metalation of the fused pyridine (I) followed by electrophilic quench allows the preparation
of p-substituted derivatives. The bromide (X) is utilized in the synthesis of compounds
such as (XIII), which shows moderate potent binding affinity for the CRF1 receptor.
— (HARTZ*, R. A.; NANDA, K. K.; INGALLS, C. L.; Tetrahedron Lett. 46 (2005)
10, 1683-1686; Discovery Chem., Bristol-Myers Squibb Pharm. Res. Inst.,
Wallingford, CT 06492, USA; Eng.) — Mais
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