1072895-86-3Relevant articles and documents
Discovery of dual orexin receptor antagonists with rat sleep efficacy enabled by expansion of the acetonitrile-assisted/diphosgene-mediated 2,4-dichloropyrimidine synthesis
Roecker, Anthony J.,Mercer, Swati P.,Harrell, C. Meacham,Garson, Susan L.,Fox, Steven V.,Gotter, Anthony L.,Prueksaritanont, Thomayant,Cabalu, Tamara D.,Cui, Donghui,Lemaire, Wei,Winrow, Christopher J.,Renger, John J.,Coleman, Paul J.
, p. 2079 - 2085 (2014/05/06)
Recent clinical studies have demonstrated that dual orexin receptor antagonists (OX1R and OX2R antagonists or DORAs) represent a novel treatment option for insomnia patients. Previously we have disclosed several compounds in the diazepane amide DORA series with excellent potency and both preclinical and clinical sleep efficacy. Additional SAR studies in this series were enabled by the expansion of the acetonitrile-assisted, diphosgene-mediated 2,4-dichloropyrimidine synthesis to novel substrates providing an array of Western heterocycles. These heterocycles were utilized to synthesize analogs in short order with high levels of potency on orexin 1 and orexin 2 receptors as well as in vivo sleep efficacy in the rat.
A novel strategy for the synthesis of uracil derivatives using bis(pentafluorophenyl)imidodicarbonate
Chichetti, Stephanie M.,Ahearn, Sean P.,Rivkin, Alexey
scheme or table, p. 6081 - 6083 (2009/04/04)
The disclosure herein describes a novel strategy for the synthesis of uracil derivatives via a solvent-free microwave cyclocondensation reaction using bis(pentafluorophenyl)imidodicarbonate.
