767-80-6

Usage

Preparation

synthesis of 5-Fluorobarbituric acid: Urea (1.50 g, 25 mmol) was added to the solution of sodium (1.2 g, 53 mmol) in anhydrous ethanol (50 mL) and the mixture was heated to reflux. Diethyl 2-fluoromalonate (4.45 g, 25 mmol) was added dropwise over 10 minutes and the mixture was heated at reflux for 1h. After cooling to room temperature, the solution was filtered, the residue was washed with ethanol (20 mL), dissolved in water (30 mL) and acidified with HCl to pH 1. The precipitated product was recrystallized from the liquor to afford 5-fluorobarbituric acid (1.87 g, 51%) as a tan powder.m.p.: >300 °C; ([M + H]+ , 147.0206, C4H4FN2O3 requires: [M]+ , 147.0204); IR (neat,cm-1 ) 2926, 2828, 1578, 1383, 1241, 1128; δF (D2O + NaOD, 376 MHz): -191.95 (s); δC (D2O + NaOD, 100 MHz) 131.89 (d, 1 JCF 214.4, C-F), 157.77 (d, 4 JCF 6.2, C-NH), 164.59 (d, 2 JCF 13.4, CvO); m/z (ASAP) 147 (25%, [M + H]+ ).18a

Upstream product

• 685-88-1 fluoromalonic acid diethyl ester 
• 57-13-6 urea 
• 67-52-7 BARBITURIC ACID 
• 344-14-9 dimethyl 2-fluoromalonate 

Downstream Products

• 1192479-36-9 2-chloro-5-fluoro-4,6-dimethylpyrimidine 

Relevant academic research and scientific papers

COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, COMPOSITION FOR ORGANIC OPTOELECTRONIC DEVICE AND ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE

The present specification relates to a compound for an organic optoelectronic device represented by chemical formula 1, a composition for an organic optoelectronic device including the same, an organic optoelectronic device, and a display device. Details

Heterocyclic Compound

The present invention provide a compound having an orexin receptor antagonistic activity, which is expected to be useful as medicaments such as agents for the prophylaxis or treatment of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease and the like. The present invention relates to a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof.

Fluorine gas for life science syntheses: Green metrics to assess selective direct fluorination for the synthesis of 2-fluoromalonate esters

Optimisation and real time reaction monitoring of the synthesis of 2-fluoromalonate esters by direct fluorination using fluorine gas is reported. An assessment of green metrics including atom economy and process mass intensity factors, demonstrates that the one-step selective direct fluorination process compares very favourably with established multistep processes for the synthesis of fluoromalonates.

PEPTIDE DEFORMYLASE INHIBITORS

The present invention relates to {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3- oxopropyl}hydroxyformamide compounds of Formula (I): or pharmaceutically acceptable salts thereof, corresponding pharmaceutical compositions, processes for making and use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity and in treatment methods for bacterial infections

DISUBSTITUTED OCTAHY-DROPYRROLO [3,4-C] PYRROLES AS OREXIN RECEPTOR MODULATORS

Disubstituted octahydropyrrolo[3,4-c]pyrrole compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.

FUSED HETEROCYCLIC COMPOUNDS AS OREXIN RECEPTOR MODULATORS

Certain disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane are described, which are useful as orexin inhibitors. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.

FUSED HETEROCYCLIC COMPOUNDS AS OREXIN RECEPTOR MODULATORS

Disubstituted 3,8-diaza-bicyclo[4.2.0]octane and 3,6-diazabicyclo [3.2.0]heptane compounds are described, which are useful as orexin receptor modulators. Such compounds may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia.

PEPTIDE DEFORMYLASE INHIBITORS

The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives, compositions containing them, the use of such compounds in the inhibition of bacterial peptide deformylase (PDF) activity, and in the treatment of bacterial infections. Specifically, the invention is directed to compounds of formula (I), wherein R1, R2 and R3 are defined herein and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.

Direct Fluorination of 1,3-Dicarbonyl Compounds

1,3-Dicarbonyls, such as 1,3-diketones and 1,3-ketoesters, react directly with elemental fluorine at room temperature to give the corresponding 2-fluoro- and, in some cases, 2,2-difluoro-compounds in high yield.

A NOVEL ROUTE TO 5-FLUOROURACILS FROM CHLOROTRIFLUOROETHENE

Diethyl fluoromalonate was prepared in one-pot from chlorotrifluoroethene via trifluoroacrylic acid lithium salt in 79percent yield.Diethyl fluoromalonate was easily converted to 5-fluoro-6-chlorouracils, reductions of which gave 5-fluorouracils in good yields.