84328-69-8

Upstream product

• 16588-15-1 2-chloro-5-nitro-benzamide 
• 2516-96-3 2-chloro-5-nitrobenzoic acid 
• 75-89-8 2,2,2-trifluoroethanol 
• 16588-02-6 4-chloro-3-cyanonitrobenzene 
• 420-87-1 sodium 2,2,2-trifluoroethanolate 

Downstream Products

• 288249-65-0 N-[3-cyano-4-(2,2,2-trifluoroethyl)phenyl]-1-(4-fluorophenyl)pyrrole-3-carboxamide 
• 288252-09-5 5-amino-2-(4-tert-butyldimethylsilyloxypiperidino)benzonitrile 
• 288252-08-4 5-amino-2-(2,2,2-trifluoroethoxy)benzonitrile 

Relevant academic research and scientific papers

Anti-enteroviral activity of new MDL-860 analogues: Synthesis, in vitro/in vivo studies and QSAR analysis

A series of 60 nitrobenzonitrile analogues of the anti-viral agent MDL-860 were synthesized (50 of which are new) and evaluated for their activity against three types of enteroviruses (coxsackievirus B1, coxsackievirus B3 and poliovirus 1). Among them, six diaryl ethers (20e, 27e, 28e, 29e, 33e and 35e) demonstrated high in vitro activity (SI > 50) towards at least one of the tested viruses and very low cytotoxicity against human cells. Compound 27e possesses the broadest spectrum of activity towards all tested viruses in the same way as MDL-860 does. The most active derivatives (27e, 29e and 35e) against coxsackievirus B1 were tested in vivo in newborn mice experimentally infected with 20 MLD50 of coxsackievirus B1. Compound 29e showed promising in vivo activity (protection index 26% and 4 days lengthening of mean survival time). QSAR analysis of the substituent effects on the in vitro cytotoxicity (CC50) and anti-viral activity of the nitrobenzonitrile derivatives was carried out and adequate QSAR models for the anti-viral activity of the compounds against poliovirus 1 and coxsackievirus B1 were constructed.

AMIDE COMPOUNDS AND MEDICINAL USE THEREOF

The present invention relates to a compound of the formula wherein R1 is substituted aryl, heteroaryl and the like, R2 and R3 are hydrogen, alkyl, halogen, hydroxyl group and the like, Q is N, CH and the like, W is hydrogen, alkyl, hydroxycarbonylalkyl and the like, X is halogen, cyano, nitro, amino and the like, X' is hydrogen, halogen, cyano, nitro, and Y is alkyl, hydroxyl group, alkoxy, mercapto and the like and a salt thereof, and a medicine containing the said compound. The compound of the present invention shows a superior inhibitory effect on activated lymphocytes proliferation and is useful as an agent for the prophylaxis or treatment of various autoimmune diseases.

Aromatic Fluoroalkoxylation via Direct Aromatic Nucleophilic Substitution

The reaction of activated aryl and heteroaryl halides with fluorinated alkoxide anions is described.In all cases, substitution of the halogen by a fluoroalkoxy group was observed.The effect of solvent, time, temperature, the activating group, leaving group, and the nucleophile on this reaction is also discussed.