Caron, Stephane; Do, Nga M.; Sieser, Janice E.; Whritenour, David C.; Hill, Paul D. published the artcile< Preparation of a Corticotropin-Releasing Factor Antagonist by Nucleophilic Aromatic Substitution and Copper-Mediated Ether Formation>, Formula: C9H9Cl2NO2, the main research area is butylamino aryloxy nicotinate preparation process development drug candidate; corticotropin releasing factor antagonist preparation process development drug candidate; nucleophilic aromatic substitution ether formation copper drug candidate preparation.
Several synthetic approaches to a corticotropin-releasing factor (CRF) antagonist containing a tetrasubstituted pyridine (I) were evaluated. In particular, nucleophilic aromatic substitutions on 2,4-dichloropyridine derivatives were attempted using 2,6-dimethyl-4-chlorophenol, (S)-2-aminobutanol, and several sulfur nucleophiles. It was found that a copper-mediated coupling of a phenoxymesylate was preferred for preparation of the diarylether followed by nucleophilic aromatic substitution to introduce the amine side chain, affording the desired drug candidate (I) in two steps from the com. available Me 2,4-dichloro-6-methylnicotinate.
Organic Process Research & Development published new progress about Etherification. 86129-63-7 belongs to class pyridine-derivatives, and the molecular formula is C9H9Cl2NO2, Formula: C9H9Cl2NO2.