1841-49-2

Upstream product

• 446-08-2 2-amino-5-fluorobenzoic acid 
• 106-39-8 bromochlorobenzene 
• 880875-39-8 2-amino-5-fluoro-N-methoxy-N-methylbenzamide 
• 1588428-56-1 3-(4-chlorophenyl)-5-fluoro-3-hydroxyindolin-2-one 
• 321-69-7 5-fluoroisatoic anhydride 

Downstream Products

• 138772-94-8 <(S)->N-isonicotinoyl-2-amino-4'-chloro-5-fluorobenzhydrol 
• 1449372-97-7 3-acetyl-4-(4-chlorophenyl)-6-fluoroquinolin-2(1H)-one 
• 1449373-35-6 (E)-4-(4-chlorophenyl)-3-[3-(4-chlorophenyl)acryloyl]-6-fluoroquinolin-2(1H)-one 
• 1449373-79-8 4-(4-chlorophenyl)-3-[5-(4-chlorophenyl)-4,5-dihydro-1H-pyrazol-3-yl]-6-fluoroquinolin-2(1H)-one 
• 1449374-22-4 4-{5-(4-chlorophenyl)-3-[4-(4-chlorophenyl)-6-fluoro-2-oxo-1,2-dihydroquinolin-3-yl]-4,5-dihydro-1H-pyrazol-1-yl}-4-oxobutanoic acid 
• 91715-21-8 Sodium; [2-amino-3-(4-chloro-benzoyl)-5-fluoro-phenyl]-acetate 
• 91714-21-5 7-(4-Chloro-benzoyl)-5-fluoro-3-methylsulfanyl-1,3-dihydro-indol-2-one 
• 91714-22-6 7-(4-Chloro-benzoyl)-5-fluoro-1,3-dihydro-indol-2-one 
• 138772-92-6 <(S)->2-amino-4'-chloro-5-fluorobenzhydrol 

Relevant academic research and scientific papers

One-Pot Synthesis of 2-Aminobenzophenones from 2-Alkynyl Arylazides Catalyzed by Pd and Cu Precursors

We describe a novel one-pot three-step reaction of 2-alkynyl arylazides through palladium-catalyzed formation of 3-hydroxy-3-phenylindolin-2-ones followed by hydrolysis of amide bonds and copper-catalyzed decarboxylation to give 2-aminobenzophenones. This synthetic method works well with various 2-alkynyl arylazides and affords the products in moderate to good yields under mild reaction conditions.

Structure-activity relationships and pharmacophore model of a noncompetitive pyrazoline containing class of GluN2C/GluN2D selective antagonists

Here we describe the synthesis and structure-activity relationship for a class of pyrazoline-containing dihydroquinolone negative allosteric modulators of the NMDA receptor that show strong subunit selectivity for GluN2C- and GluN2D-containing receptors over GluN2A- and GluN2B-containing receptors. Several members of this class inhibit NMDA receptor responses in the nanomolar range and are more than 50-fold selective over GluN1/GluN2A and GluN1/GluN2B NMDA receptors, as well as AMPA, kainate, GABA, glycine, nicotinic, serotonin, and purinergic receptors. Analysis of the purified enantiomers of one of the more potent and selective compounds shows that the S-enantiomer is both more potent and more selective than the R-enantiomer. The S-enantiomer had an IC 50 of 0.17-0.22 μM at GluN2D- and GluN2C-containing receptors, respectively, and showed over 70-fold selectivity over other NMDA receptor subunits. The subunit selectivity of this class of compounds should be useful in defining the role of GluN2C- and GluN2D-containing receptors in specific brain circuits in both physiological and pathophysiological conditions.