5676-60-8

Usage

Chemical Properties

Light brown powder

InChI:InChI=1/C8H8N2O/c1-5-10-7-3-2-6(9)4-8(7)11-5/h2-4H,9H2,1H3

Upstream product

• 95-21-6 2-methyl-1,3-benzoxazole 
• 5683-43-2 2-methyl-6-nitrobenzoxazole 
• 110-54-3 hexane 
• 7439-89-6 iron 
• 121-88-0 5-Nitro-2-aminophenol 
• 13452-14-7 2-methyl-6-benzoxazole carboxylic acid 

Downstream Products

• 59997-00-1 N,N'-(hydroxy-p-phenylene)-bis-acetamide 
• 686747-44-4 2,5-dichloro-N-(2-methylbenzooxazol-6-yl)benzenesulfonamide 
• 686747-43-3 N-(2-methylbenzooxazol-6-yl)-4-propylbenzenesulfonamide 
• 686747-42-2 3-chloro-2-methyl-N-(2-methylbenzooxazol-6-yl)benzenesulfonamide 

Relevant academic research and scientific papers

Synthesis of 9,10-distyrylanthracene derivative and its one- and two-photon induced emission in solid state

Solid fluorescence plays an important role in optoelectronic devices. In this paper, 9,10-bis(6-dimethylamino benzoxazole styryl)-anthracene (1) was synthesized. 1 displayed a strong emission in solid state (microcrystalline state, amorphous solid state and polymeric thin film) resulted from aggregation-induced emission mechanism, and a large absolute fluorescence quantum yield (?f = 0.65) was obtained. 1 also exhibited up-conversion emission in solid state and a strong yellow emission was observed upon excitation with 800–1064 nm, the quadratic dependence of the fluorescence on the excitation laser intensity confirmed that the up-conversion emission resulted from two-photon process.

Design, synthesis and biological evaluation of novel Pseudomonas aeruginosa DNA gyrase B inhibitors

In the present study, we attempted to develop a novel class of compounds active against Pseudomonas aeruginosa (Pa) by exploring the pharmaceutically well exploited enzyme targets. Since, lack of Pa gyrase B crystal structures, Thermus thermophilus gyrase B in complex with novobiocin (1KIJ) was used as template to generate model structure by performing homology modeling. Further the best model was validated and used for high-throughput virtual screening, docking and dynamics simulations using the in-house database for identification of Pa DNA gyrase B inhibitors. This study led to an identification of three lead molecules with IC50 values in range of 6.25–15.6 μM against Pa gyrase supercoiling assay. Lead-1 optimization and expansion resulted in 15 compounds. Among the synthesized compounds six compounds were shown good enzyme inhibition than Lead-1 (IC50 6.25 μM). Compound 13 emerged as the most potential compound exhibiting inhibition of Pa gyrase supercoiling with an IC50 of 2.2 μM; and in-vitro Pa activity with MIC of 8 μg/mL in presence of efflux pump inhibitor; hence could be further developed as novel inhibitor for Pa gyrase B.

NOVEL NICOTINAMIDE DERIVATIVES OR SALTS THEREOF

An object of the present invention is to provide to a compound and a pharmaceutical composition, which have excellent Syk-inhibitory activity. Th e present invention provides a nicotinamide derivative represented by the follo wing formula (I) (wherein R 1 represents a halogen atom; R 2 represents a C 1-12 alkyl group, a C 2-12 alkenyl group, a C 2-12 alkynyl group, a C 3-8 cycloalkyl g roup, an aryl group, an ar-C 1-6 alkyl group or a heterocyclic group, each opti onally having at least one substituent; R 3 represents an aryl group or a hetero cyclic group each optionally having at least one substituent; and R 4 and R 5 e ach independently represent a hydrogen atom; and R 2 and R 4 may form a cyc lic amino group optionally having at least one substituent together with the ni trogen atom to which they bind) or a salt thereof, and a pharmaceutical comp osition for use in the treatment of a Syk-related disease which comprises the nicotinamide derivative or a salt thereof.

Palladium-catalyzed cross-coupling reaction of azides with isocyanides

An efficient palladium-catalyzed cross-coupling reaction of azides with isocyanides is developed, providing a general synthetic route to unsymmetric carbodiimides with excellent yields. This method shows a broad substrate scope, including not only aryl azides, but also unactivated benzyl and alkyl azides. Furthermore, from readily available substrates, Pd-catalyzed coupling with a tandem amine insertion cascade to obtain unsymmetric trisubstituted guanidines has been achieved in a one-pot fashion.

Iron-catalysed, general and operationally simple formal hydrogenation using Fe(OTf)3 and NaBH4

An operationally simple and environmentally benign formal hydrogenation protocol has been developed using highly abundant iron(iii) salts and an inexpensive, bench stable, stoichiometric reductant, NaBH4, in ethanol, under ambient conditions. This reaction has been applied to the reduction of terminal alkenes (22 examples, up to 95% yield) and nitro-groups (26 examples, up to 95% yield). Deuterium labelling studies indicate that this reaction proceeds via an ionic rather than radical mechanism.

PHTHALAZINONE COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS

The invention relates to a compound of Formula I and methods of treating CFTR (cystic fibrosis transmembrane conductance regulator) mediated diseases, in particular cystic fibrosis, comprising the step of administering a therapeutically effective amount o

SUBSTITUTED ARYLSULFONYLAMINOMETHYLPHOSPHONIC ACID DERIVATIVES, THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF TYPE I AND II DIABETES MELLITUS

The present invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein R, X, Y and Z are defined as in claim 1, the tautomers, enantiomers, diastereomers, mixtures thereof and salts thereof which ha

NEW GPR119MODULATORS

The application relates to compounds of Formula (Ia): and pharmaceutically acceptable salts, solvates, hydrates, geometrical isomers, tautomers, optical isomersor N-oxides thereof. The application also relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the prophylaxis and treatment of medical conditions relating to disorders of the G-protein- coupled receptor GPR119, such as diabetes, obesity and osteoporosis.

METHOD FOR THE PREPARATION OF FUSED HETEROCYCLIC SUCCINIMIDE COMPOUNDS AND ANALOGS THEREOF

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.

Fused heterocyclic succinimide compounds and analogs thereof, modulators of nuclear hormone receptor function

Fused cyclic compounds, methods of using such compounds in the treatment of nuclear hormone receptor-associated conditions such as cancer and immune disorders, and pharmaceutical compositions containing such compounds.