245554-82-9

Upstream product

• 7194-78-7 (3-bromophenyl)oxoacetic acid 
• 95-54-5 1,2-diamino-benzene 
• 81316-36-1 methyl (m-bromophenyl)glyoxylate 
• 98042-29-6 2,2-dibromo-1-(3-bromophenyl)ethan-1-one 
• 2142-63-4 1-(3-Bromophenyl)ethanone 
• 62123-80-2 ethyl 2-(3-bromo-phenyl)-2-oxo-acetate 
• 245554-81-8 3-(3-bromophenyl)-3,4-dihydro-1H-quinoxalin-2-one 

Downstream Products

• 1152134-31-0 C₂₅H₂₆BrN₃O₅ 
• 745018-47-7 3-{4-[5-((2S,6R)-2,6-dimethylpiperidin-1-yl)pentyl]-3-oxo-3,4-dihydroquinoxalin-2-yl}benzonitrile 
• 245554-84-1 3-[4-(5-bromopentyl)-3-oxo-3,4-dihydroquinoxalin-2-yl]benzonitrile 
• 245554-83-0 3-(3-oxo-3,4-dihydroquinoxalin-2-yl)benzonitrile 

Relevant academic research and scientific papers

α-Keto Acids as Triggers and Partners for the Synthesis of Quinazolinones, Quinoxalinones, Benzooxazinones, and Benzothiazoles in Water

A general and efficient method for the synthesis of quinazolinones, quinoxalinones, benzooxazinones, and benzothiazoles from the reactions of α-keto acids with 2-aminobenzamides, benzene-1,2-diamines, 2-aminophenols, and 2-aminobenzenethiols, respectively, is described. The reactions were conducted under catalyst-free conditions, using water as the sole solvent with no additive required, and successfully applied to the synthesis of sildenafil. More importantly, these reactions can be conducted on a mass scale, and the products can be easily purified through filtration and washing with ethanol (or crystallized).

High-Potency Phenylquinoxalinone Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) Activators

We previously identified phenylquinoxalinone CFTRact-J027 (4) as a cystic fibrosis transmembrane conductance regulator (CFTR) activator with an EC50 of ～200 nM and demonstrated its therapeutic efficacy in mouse models of constipation. Here, structure-activity studies were done on 36 synthesized phenylquinoxalinone analogs to identify compounds with improved potency and altered metabolic stability. Synthesis of the phenylquinoxalinone core was generally accomplished by condensation of 1,2-phenylenediamines with substituted phenyloxoacetates. Structure-activity studies established, among other features, the privileged nature of a properly positioned nitro moiety on the 3-aryl group. Synthesized analogs showed improved CFTR activation potency compared to 4 with EC50 down to 21 nM and with greater metabolic stability. CFTR activators have potential therapeutic indications in constipation, dry eye, cholestatic liver diseases, and inflammatory lung disorders.

BISMACROKYCLIC COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS

The present invention discloses compounds of formula (Ia) or (Ib) or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequent

QUINOXALINE-CONTAINING COMPOUNDS AS HEPATITIS C VIRUS INHIBITORS

The present invention discloses compounds of formula I and II or pharmaceutically acceptable salts, esters, or prodrugs thereof which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, t

Design, synthesis, and biological activity of potent and selective inhibitors of blood coagulation factor Xa

Factor Xa (FXa) has materialized as a key enzyme for the intervention of the blood coagulation cascade and for the development of new antithrombotic agents. FXa is the lone enzyme responsible for the production of thrombin and therefore is an attractive t