21732-93-4

Upstream product

• 15944-74-8 3,6-dichloro-2-nitro-aniline 
• 65036-57-9 1,4-dichloro-2,3-dinitrobenzene 
• 89-61-2 2,5-dichloronitrobenzene 
• 273-13-2 benzo[1,2,5]thiadiazole 
• 2207-34-3 4,7-dichlorobenzo[c][1,2,5]thiadiazole 

Downstream Products

• 94544-96-4 5,8-dichloro-2,3-diphenyl-quinoxaline 
• 1196131-60-8 4,7-dichloro-2-(4-fluorophenyl)-1H-benzimidazole 
• 1225652-20-9 5,8-dichloro-2-methyl-3-[3'-(methylsulfonyl)biphenyl-4-yl]quinoxaline 
• 102466-68-2 3-(4,7-dichloro-benzotriazol-2-yl)-1,3-diphenyl-propan-1-one 

Relevant academic research and scientific papers

Programmed Sequential Additions to Halogenated Mucononitriles

Dihalomucononitriles were synthesized and their reactivity evaluated to assess their ability to function as linchpin reagents. Bis(2-chloroacrylonitrile) and bis(2-bromoacrylonitrile) were synthesized from 2,1,3-benzothiadiazole and undergo conjugate addition/elimination reactions with both nitrogen (40-95% yield) and carbon nucleophiles (72-93% yield). Secondary amines undergo monosubstitutions, while carbon nucleophiles are added twice. The sequence of addition of the nucleophiles could be controlled to give mixed addition products. The multicomponent coupling products could then be converted to natural product like motifs using intramolecular cyclization reactions.

HETEROARYL COMPOUNDS AND METHODS OF USE THEREOF

Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes

Synthesis and potent antifungal activity against Candida species of some novel 1H-benzimidazoles

(Chemical Equation Presented) A series of 47 novel N1-alkylated- 2-aryl-5(6)-substituted-1H-benzimidazoles and their three novel indole analogues were synthesized and evaluated for in vitro antifungal activities against Candida species by the tube dilution method. The results showed that compounds 79 and 80, having pyridine at the position C-2, of benzimidazoles exhibited the greatest activity with MIC values of 6.25-3.12 μg/mL. Indole analogues 108-110 have no inhibitory activity.

Potent Quinoxaline-Spaced Phosphono α-Amino Acids of the AP-6 Type as Competitive NMDA Antagonists: Synthesis and Biological Evaluation

A series of α-amino-3-(phosphonoalkyl)-2-quinoxalinepropanoic acids was synthesized and evaluated for NMDA receptor affinity using a CPP binding assay.Functional antagonism of the NMDA receptor complex was evaluated in vitro using a stimulated TCP binding assay and in vivo by empolying an NMDA-induced seizure model.Some analogues also were evaluated in the -glycine binding assay.Several compounds of the AP-6 type show potent and selective NMDA antagonistic activity both in vitro and in vivo.In particular α-amino-7-chloro-3-(phosphonomethyl)-2-quinoxalinepropanoic acid (1) d isplayed an ED50 of 1.1 mg/kg ip in the NMDA lethality model.Noteworthy is α-amino-6,7-dichloro-3-(phosphonomethyl)-2-quinoxalinepropanoic acid (3) with a unique dual activity, displaying in the NMDA receptor binding assay an IC50 of 3.4 nM and in the glycine binding assay an IC50 of 0.61 μM.