Synthesis of the kappa-agonist CJ-15,161 via a palladium-catalyzed cross-coupling reaction.
Syntheses of CJ-15,161 (1) involving intermolecular N-arylation of an appropriately functionalized diamine, obtained from the precursor alpha-amino acids or, more conveniently, from the corresponding 1,2-amino alcohols via 1,2,3-oxathiazolidine-2,2-dioxide 22, are reported.
Ghosh
Arun
A
Chemical Research and Development, Pfizer Global Research and Development, Eastern Point Road, P.O. Box 8013, Groton, CT 06340-8013, USA. Arun_Ghosh@groton.pfizer.com
Sieser
Janice E
JE
Caron
Stéphane
S
Watson
Timothy J N
TJ
D002384:Catalysis; D007202:Indicators and Reagents; D008024:Ligands; D010165:Palladium; D011759:Pyrrolidines; D017473:Receptors, Opioid, kappa / Q000819:agonists*
D007202:Indicators and Reagents; D008024:Ligands; D011759:Pyrrolidines; D017473:Receptors, Opioid, kappa; C464962:CJ-15161; D010165:Palladium