193217-46-8Relevant articles and documents
Iron-catalyzed stereospecific arylation of enol tosylates using Grignard reagents
Wei, Yi-Ming,Ma, Xiao-Di,Wang, Lei,Duan, Xin-Fang
supporting information, p. 1101 - 1104 (2020/02/04)
The stereospecific Fe-catalyzed arylation of enol tosylates was reported. Various tri- or tetrasubstituted Z or E-enol tosylates of β-keto esters were arylated using common and Knochel-type Grignard reagents with complete stereofidelity. The precursors fo
Chromeno[3,4-c]pyridin-5-ones: Selective human dopamine D4 receptor antagonists as potential antipsychotic agents
Unangst, Paul C.,Capiris, Thomas,Connor, David T.,Heffner, Thomas G.,MacKenzie, Robert G.,Miller, Steven R.,Pugsley, Thomas A.,Wise, Lawrence D.
, p. 2688 - 2693 (2007/10/03)
The discovery of a series of chromeno[3,4-c]pyridin-5-ones with selective affinity for the dopamine D4 receptor is described. Target compounds were tested for binding to cloned human dopamine D2, D3 and D4 receptor subtypes expressed in Chinese hamster ovary (CHO) K-1 cells. Several compounds demonstrated single digit nanomolar K(i) values for binding to the D4 receptor with several hundred-fold selectivities toward the D2 and D3 receptors. A limited SAR study of this series is discussed. In a mitogenesis assay measuring [3H]thymidine uptake, the target compounds showed antagonist to weak, partial agonist activity at the D4 receptor, with intrinsic activities ranging from 0 to 35%. Compound 6, 3-benzyl-8-methyl-1,2,3,4- tetrahydrochromeno[3,4-c]pyridin-5-one, increased DOPA (L-3 4- dihydroxyphenylalanine) synthesis 84% in the hippocampus and 10% in the striatum of rat brain when dosed orally at 10 mg/kg.