Design of a serotonin 4 receptor radiotracer with decreased lipophilicity for single photon emission computed tomography

Combinatorial Chemistry Online Volume 17, Issue 7, July 2015

“…A preferred compound exhibited a binding affinity value of 0.094 nM toward human 5-HT4R and high selectivity over other serotonin receptor subtypes. In vivo SPECT imaging studies and competition experiments demonstrated that decreased lipophilicity compared with earlier compounds allowed a more specific labelling of the 5-HT4R brain-containing regions [20].…”

Radiotracers for the Central Serotoninergic System

“…All these ligands belong to the same family of compounds and contain an ester function which can generate short metabolic stability. Other chemical series deprived of ester functions have been explored recently, such as azaphenanthrene derivatives [ 210 ].…”

AlCl3-Promoted Intramolecular Indolinone-Quinolone Rearrangement of Spiro[indoline-3,2′-quinoxaline]-2,3′-diones: Easy Access to Quinolino[3,4-b]quinoxalin-6-ones

“…Zhang et al developed a facile and direct intramolecular oxidative C­(aryl)-H amidation reaction for the synthesis of quinolino­[3,4- b ]­quinoxalin-6­(5 H )-ones in moderate to excellent yields starting from readily available materials by tethering the adjacent N -methoxyamide and aryl portions in the presence of phenyliodine­(III) bis­(trifluoroacetate) at room temperature (Scheme f) . Moreover, the cross-combination of 3-chloro-2-cyanopyrazine with boron compounds resulted in the production of biaryl derivatives followed by the closure of the anion cycle in the presence of 5 KOH equivalents in a sealed tube containing t -BuOH at 150 °C to obtain the target pyrazino [2,3- c ]­quinolin-5­(6 H )-ones in a two-stage reaction. , …”