22280-62-2

Usage

Chemical Properties

Light yellow Cryst

InChI:InChI=1/C6H7N3O2/c1-4-5(9(10)11)2-3-6(7)8-4/h2-3H,1H3,(H2,7,8)/p+1

Upstream product

• 1824-81-3 2-Amino-6-methylpyridine 
• 18605-16-8 6-fluoro-2-methyl-3-nitro-pyridine 
• 109-06-8 α-picoline 
• 33986-37-7 6-methyl-2-nitraminopyridine 
• 7664-93-9 sulfuric acid 

Downstream Products

• 22280-60-0 6-chloro-4-methyl-3-nitropyridine 
• 28489-45-4 6-methyl-5-nitropyridin-2-ol 
• 56960-81-7 2-Amino-3-chlor-6-methyl-5-nitro-pyridin 
• 150935-62-9 2-amino-3-bromo-6-methyl-5-nitropyridine 
• 158980-19-9 ethyl 5-methyl-6-nitroimidazo<1,2-a>pyridine-2-carboxylate 
• 5467-69-6 6-methoxy-3-nitro-2-picoline 
• 28489-37-4 (6-methyl-5-nitro-[2]pyridyl)-hydrazine 
• 15367-28-9 benzaldehyde-(6-methyl-5-nitro-[2]pyridylhydrazone) 
• 28489-45-4 6-methyl-5-nitropyridin-2(1H)-one 
• 6992-84-3 6-methyl-pyridine-2,5-diyldiamine 
• 57207-96-2 3-tert. butyl-5-nitro-6-methyl-N-(5'-nitro-6'-methylpyrid-2'-yl) salicylamide 
• 57187-74-3 3-tert. butyl-5-nitro-N-(5'-nitro-6'-methylpyrid-2'-yl)salicylamide 
• 573764-90-6 5-methylimidazo[1,2-a]pyridin-6-amine 
• 52310-50-6 5-methyl-6-nitroimidazo[1,2-a]pyridine 

Relevant academic research and scientific papers

Syntheses and pharmacokinetic evaluations of four metabolites of 2-(4-(2-((1H-benzo[d]imidazol-2-yl)thio)ethyl)piperazin-1-yl)-N-(6-methyl-2,4-bis-(methylthio)pyridin-3-yl)acetamide hydrochloride [K-604], an acyl-CoA:cholesterol O-acyltransferase-1 inhibi

We synthesized and identified four metabolites of acyl-coenzyme A:cholesterol O-acyltransferase (ACAT)-1 inhibitor, K-604 (1). Two of the metabolites M1 and M2, were prepared from 1 using a combination reagent of hydrogen peroxide and sodium tungstate wit

Preparation method of 2-amino substituted six-membered nitrogen-containing heterocycle complex

The invention discloses a preparation method of a 2-amino substituted six-membered nitrogen-containing heterocycle complex. The preparation method comprises the following steps: mix 2-fluorine substituted six-membered nitrogen-containing heterocycle complex and amidine hydrochloride salt compound, and then react under the action of a alkaline substance to obtain a 2-amino substituted six-memberednitrogen-containing heterocycle complex. Preferably, the 2-amino substituted six-membered nitrogen-containing heterocycle complex is a 2-amino pyridine compound, a 2-aminopyrimidine compound or a 2-aminopyrazine compound. Compared with the prior art, the method has the advantages of simple synthesis conditions, less reaction steps, mild reaction conditions, low cost of the catalyst used, less waste discharge and good functional group tolerance.

Transition-metal-free access to 2-aminopyridine derivatives from 2-fluoropyridine and acetamidine hydrochloride

Under catalyst-free conditions, an efficient method for the synthesis of 2-aminopyridine derivatives through the nucleophilic substitution and hydrolysis of 2-fluoropyridine and acetamidine hydrochloride has been developed. This amination uses inexpensive acetamidine hydrochloride as the ammonia source and has the advantages of a high yield, high chemoselectivity and wide substrate adaptability. The results suggest that other N-heterocycles containing fluorine substituents can also complete the reaction via these reaction conditions and yield the target products.

Ethanol compound used as FGFR inhibitor

The invention discloses an ethanol compound used as a FGFR inhibitor. The invention provides the compound as shown in a formula I which is described in the specification or a pharmaceutically acceptable salt thereof, a preparation method for the compound and application of the compound as a medicine to treatment of cancers.

Identification of novel inhibitors of Aurora A with a 3-(pyrrolopyridin-2-yl)indazole scaffold

A novel series of 3-(pyrrolopyridin-2-yl)indazole derivatives were synthesized and biologically evaluated for their anti-proliferative effects on five human cancer cell lines. As a result, all of them exhibited vigorous potency against HL60 cell line with IC50 values ranging from singe digital nanomolar to micromolar level. Besides, a majority of them displayed modest to good antiproliferative activities against the other four cell lines, including KB, SMMC-7721, HCT116, and A549. Particularly, compound 2y, as the most distinguished one in this series, demonstrated IC50 values of 8.3 nM and 1.3 nM against HL60 and HCT116 cell lines, respectively. Afterwards, for exploring the molecular target, compounds2d, 2g and 2y were further selected to evaluate the inhibitory activities against a panel of kinases. Finally, they were identified to be targeting Aurora A kinase with significant selectivity over other kinases, such as CHK1, CDK2, MEK1, GSK3β, BRAF, IKKβ and PKC.

Theoretical and experimental NMR data of 3,5-dinitro-2-(2-phenylhydrazinyl) pyridine and of its 4- and 6-methyl derivatives

3,5-Dinitro-2-(2-phenylhydrazinyl)pyridine and its methyl derivatives: 4-methyl-3,5-dinitro-2-(2-phenylhydrazinyl)pyridine and 6-methyl-3,5-dinitro-2- (2-phenylhydrazinyl)pyridine were synthesized and characterized by 1H NMR and 13C NMR. Calculations were also performed where the above molecules were optimized using the methods of density functional theory (DFT) with 6-31G(d,p) and 6-311G(d,p) basis sets. For all molecules studied, the lowest energy was obtained using the 6-311G(d,p) basis set. The GIAO/DFT (Gauge Invariant Atomic Orbitals/Density Functional Theory) calculations on the 6-311G and 6-311++G and 6-311G* basis sets were carried out to determine proton and carbon chemical shifts and to find they were close to the experimental values. It has been also found that intramolecular hydrogen bonding exists between hydrogen atom (in 2-NH group) and oxygen atom (pyridine-3-NO2). Moreover, resonances between pyridine ring and electron withdrawing 3-nitro group as well between that ring and the lone electron pair of NH group favor a co-planarity of the structure; this means a chelate ring created by above-mentioned intramolecular hydrogen bond is almost co-planar with pyridine ring.

Synthesis of some fluorine-containing pyridinealdoximes of potential use for the treatment of organophosphorus nerve-agent poisoning

Fluoroheterocyclic aldoximes were screened as therapeutic agents for the treatment of anticholinesterase poisoning. 2-Fluoropyridine-3- and -6-aldoxime, and 3-fluoropyridine-2- and -4-aldoxime, were synthesised. Attempts to obtain 3,5,6-trifluoropyridine-2,4-bis(aldoxime) and -2-aldoxime, however, proved unsuccessful. Pentafluorobenzaldoxime was prepared by oximation of pentafluorobenzaldehyde. Acid dissociation constants (pKa) and second-order rate constants (kox-) of the fluorinated pyridinealdoximes towards sarin were measured. 2,3,5,6-Tetrafluoropyridine-4- aldoxime had the best profile: its kox- approached that of the therapeutic oxime P2S (310 vs. 120 l mol-1 min-1), but its higher pKa (9.1 vs. 7.8) fell short of the target figure of 8 required for reactivation of inhibited acetylcholinesterase in vivo. N-alkylation of the fluorinated pyridine-aldoximes may reduce their pK a nearer to 8 and enhance their therapeutic potential. Crown Copyright

AZAINDOLES AS INHIBITORS OF SOLUBLE ADENYLATE CYCLASE

The present invention relates to azaindoles of general Formula (I), a method for the production thereof, and to the us e thereof for the production of pharmaceutical compositions.

TETRAHYDROISOQUINOLINE COMPOUND AND MEDICINAL USE THEREOF

The present invention provide a tetrahydroisoquinoline compound having a superior ACAT-inhibitory activity and/or anti-oxidation action, particularly, novel compound represented by the formula (I) (wherein each symbol is as described in the specification) and a pharmaceutically acceptable salt thereof.

Discovery of heterobicyclic templates for novel metabotropic glutamate receptor subtype 5 antagonists

Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5.