The expedient synthesis of 4,2′-difluoro-5′-(7- trifluoromethylimidazo[1,2-a]pyrimidin-3-yl)biphenyl-2-carbonitrile, a GABA α2/3 agonist
An expedient regioselective synthesis of a GABA α2/3 agonist 1 is described. The key step is an efficient regioselective palladium-catalyzed coupling of 7-trifluoromethylimidazo[1,2-a]pyrimidine (5) to 5′-chloro-4,2′-difluorobiphenyl-2-carbonitrile (15).
Cameron, Mark,Foster, Bruce S.,Lynch, Joseph E.,Shi, Yao-Jun,Dolling, Ulf-H.
p. 398 - 402
(2012/12/22)
Imidazo[1,2-a]pyrimidines as functionally selective and orally bioavailable GABAAα2/α3 binding site agonists for the treatment of anxiety disorders
A series of high-affinity GABAA agonists with good oral bioavailability in rat and dog and functional selectivity for the GABA Aα2 and -α3 subtypes is reported. The 7-trifluoromethylimidazopyrimidine 14g and the 7-propan-2-olimidazopyrimidine 14k are anxiolytic in both conditioned and unconditioned animal models of anxiety with minimal sedation observed at full BZ binding site occupancy.
Goodacre, Simon C.,Street, Leslie J.,Hallett, David J.,Crawforth, James M.,Kelly, Sarah,Owens, Andrew P.,Blackaby, Wesley P.,Lewis, Richard T.,Stanley, Joanna,Smith, Alison J.,Ferris, Pushpinder,Sohal, Bindi,Cook, Susan M.,Pike, Andrew,Brown, Nicola,Wafford, Keith A.,Marshall, George,Castro, José L.,Atack, John R.
p. 35 - 38
(2007/10/03)
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