Glyoxal appears as yellow crystals melting at15°C. Hence often encountered as a light yellow liquid with a weak sour odor. Vapor has a green color and burns with a violet flame.
颜色/状态：
Yellow prisms or irregular pieces turning white on cooling; opaque at 10 °C; vapors are green
气味：
Mild odor
蒸汽密度：
greater than 1.0 (NTP, 1992) (Relative to Air)
蒸汽压力：
255 mm Hg at 25 °C /extrapolated/
亨利常数：
3.33e-09 atm-m3/mole
大气OH速率常数：
1.14e-11 cm3/molecule*sec
自燃温度：
285 °C
分解：
When heated to decomposition it emits acrid smoke and irritating fumes.
聚合：
Polymerizes...on contact with water (violent reaction), or when dissolved in solvents containing water.
The cytosolic GSH-dependent glyoxalase system is the major pathway for the detoxification of glyoxal ... Glyoxal reacts non-enzymatically with GSH with formation of a hemithioacetal, which is subsequently converted to S-glycolylglutathione by glyoxalase I. Glyoxalase II catalyses the hydrolysis of S-glycolylglutathione to glycolate, re-forming the GSH from the first reaction. The activity of glyoxalase I in situ is approximately proportional to the cytosolic concentration of GSH. When GSH is severely depleted (eg, under conditions of oxidative stress), however, 2-oxoaldehyde dehydrogenase and aldose reductase may also metabolize glyoxal. Imbalances in intracellular redox systems may impair these detoxification mechanisms, resulting in higher levels of glyoxal. A further GSH-independent route of detoxification via glyoxalase III exists.
IDENTIFICATION: Glyoxal is generally available as an aqueous solution, typically containing 30-50% glyoxal in which hydrated oligomers are present. This chemical is used as a chemical intermediate in the production of pharmaceuticals and dyestuffs, as a cross-linking agent in the production of polymers, as a biocide, and as a disinfecting agent. Due to microbial activity as well as non-enzymatic autoxidation of oil or browning reactions of saccharides, glyoxal is frequently detected in fermented food and beverages. It is found in beer, wine and tea. HUMAN EXPOSURE: The main routes of occupational exposure to glyoxal during use as a disinfectant are via inhalation and dermal absorption. The general population is exposed mainly through ingestion of glyoxal containing food, but could be exposed through polluted air in urban areas and traces of glyoxal found in drinking water. Glyoxal is endogenously produced during normal cellular metabolism by a multitude of enzyme independent pathways. Glyoxal is found in human blood and individuals with diabetes or renal failure have higher concentrations. Glyoxal is irritating to mucous membranes and acts as a skin sensitizing agent. ANIMAL/PLANT STUDIES: The acute toxicity of glyoxal in experimental animals is low to moderate, depending upon the concentration of the chemical. After inhalation exposure, local irritations of the eyes and respiratory tract as well as hyperemia and foamy secretion in the lungs predominate. After oral exposure to glyoxal, macroscopic observations include irritations to the gastrointestinal tract and congestion in the gastrointestinal tract, lung, kidney and adrenal glands. In the prominent target organs, pancreas and kidney, the toxic action of glyoxal leads to severe degenerative changes resembling those induced during diabetes. A 28 day study at high dosages of glyoxal administered to rats effects included reduced water and food intake and retardation of body weight gain. A 90 day feeding study in dogs failed to reveal any treatment related effects. Glyoxal is irritating to mucous membranes and acts as a sensitizing agent in experimental animals. Fetotoxic effects occurred only with doses of glyoxal that induced maternal toxicity. Glyoxal is directly genotoxic in vitro in bacterial and mammalian cells inducing DNA adducts, mutations, chromosomal aberrations, DNA repair, sister chromatid exchanges and DNA single strand breaks. In vivo, a genotoxic activity of glyoxal was established at the site of application in the pyloric mucosa of rats by demonstration of unscheduled DNA synthesis and DNA simple strand breaks were further observed in the rat liver. Glyoxal showed tumor promoting activity in a two stage glandular stomach carcinogenesis study in male Wistar rats, where it was inactive in a short-term liver foci assay. In an assay for tumor initiating activity of glyoxal in skin and in cell transformation assays, glyoxal yielded negative results. Exposure to glyoxal has shown to inhibit activities of aerobic and anerobic bacteria , green algae and invertebrates.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
致癌性证据
A4：不能分类为人类致癌物。
A4: Not classifiable as a human carcinogen.
来源:Hazardous Substances Data Bank (HSDB)
毒理性
暴露途径
该物质可以通过吸入其气溶胶或蒸汽以及通过摄入被身体吸收。
The substance can be absorbed into the body by inhalation of its aerosol or vapour and by ingestion.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
毒理性
皮肤症状
Redness.
Redness.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
毒理性
眼睛症状
红斑。疼痛。
Redness. Pain.
来源:ILO-WHO International Chemical Safety Cards (ICSCs)
In biological materials, less than 10% of the glyoxal present is in unbound forms in aqueous solution (free glyoxal and hydrates), as most of the reactive carbonyl groups are reversibly bound to cysteinyl, lysyl, and arginyl residues of proteins.
The endogenous concentrations of glyoxal in human tissues and body fluids, as with other alpha-oxoaldehydes, are limited by the high catalytic efficiency of the glyoxalase system as well as by the rapid reaction of glyoxal with proteins.
After acute and chronic oral administration, there is evidence of systemic absorption, with distribution to erythrocytes, liver, lung, kidney, pancreas, and adrenal glands. There is some qualitative evidence that glyoxal is absorbed after dermal exposure. Granular and vacuole degeneration in liver, kidney, and pancreas have been observed along with a distinct increase in blood glucose levels following dermal application.
Compositions for Treatment of Cystic Fibrosis and Other Chronic Diseases
申请人：Vertex Pharmaceuticals Incorporated
公开号：US20150231142A1
公开（公告）日：2015-08-20
The present invention relates to pharmaceutical compositions comprising an inhibitor of epithelial sodium channel activity in combination with at least one ABC Transporter modulator compound of Formula A, Formula B, Formula C, or Formula D. The invention also relates to pharmaceutical formulations thereof, and to methods of using such compositions in the treatment of CFTR mediated diseases, particularly cystic fibrosis using the pharmaceutical combination compositions.
[EN] IMPROVED SYNTHETIC METHODS OF MAKING (2H-1,2,3-TRIAZOL-2-YL)PHENYL COMPOUNDS AS OREXIN RECEPTOR MODULATORS<br/>[FR] PROCÉDÉS SYNTHÉTIQUES AMÉLIORÉS POUR LA FABRICATION DE COMPOSÉS DE (2H-1,2,3-TRIAZOL-2-YL)PHÉNYLE UTILISÉS COMME MODULATEURS DES RÉCEPTEURS DE L'OREXINE
申请人：JANSSEN PHARMACEUTICA NV
公开号：WO2021023843A1
公开（公告）日：2021-02-11
Processes for preparing (((3aR,6aS)-5-(4,6-dimethylpyrimidin-2-yl)hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)(2-fluoro-6-(2H-l,2,3-triazol-2- yl)phenyl)methanone are described, which are useful for commercial manufacturing. Said compound is an orexin receptor modulator and may be useful in pharmaceutical compositions and methods for the treatment of diseased states, disorders, and conditions mediated by orexin activity, such as insomnia and depression.
trifluoromethylation of N,N‐disubstituted hydrazones using the Togni reagent is demonstrated to proceed efficiently for aliphatic aldehyde‐derived substrates. The success of the reactions relied on the choice of the N,N‐diphenylamino group as the terminal hydrazone amino group where N,N‐dialkylamino groups were preferred for (hetero)aromatic aldehyde‐derived substrates. In addition, the trifluoromethylated N‐arylhydrazones
Substituted diether diols by ring-opening of carbocyclic and stannylene acetals
作者：Rolando Martínez-Bernhardt、Peter P. Castro、Gayane Godjoian、Carlos G. Gutiérrez
DOI：10.1016/s0040-4020(98)00563-8
日期：1998.7
Reduction of malonaldehyde bis(ethylene and propylene acetals) with borane or monochloroborane produces diether diols 1 and 2 in high yield. Similar reduction of glyoxal bis(ethylene acetals) has only limited utility for the preparation of tetrasubstituted triethyleneglycols 3. Organotin chemistry is complementary: stannylene acetals prepared from disubstituted vicinal diols can be alkylated with half
A Bifunctional Copper Catalyst Enables Ester Reduction with H<sub>2</sub>: Expanding the Reactivity Space of Nucleophilic Copper Hydrides
作者：Birte M. Zimmermann、Trung Tran Ngoc、Dimitrios-Ioannis Tzaras、Trinadh Kaicharla、Johannes F. Teichert
DOI：10.1021/jacs.1c09626
日期：2021.10.13
activation of esters through hydrogen bonding and formation of nucleophilic copper(I) hydrides from H2, resulting in a catalytic hydride transfer to esters. The reduction step is further facilitated by a proton shuttle mediated by the guanidinium subunit. This bifunctional approach to ester reductions for the first time shifts the reactivity of generally considered “soft” copper(I) hydrides to previously
采用基于铜 (I)/NHC 配合物和胍有机催化剂的双功能催化剂，促进了以 H 2作为末端还原剂的催化酯还原成醇。这里采用的方法能够通过氢键同时活化酯，并从 H 2形成亲核的氢化铜 (I) ，从而导致氢化物催化转移到酯。由胍亚基介导的质子穿梭进一步促进了还原步骤。这种酯还原的双功能方法首次将通常认为的“软”氢化铜 (I) 的反应性转变为以前不反应的“硬”酯亲电子试剂，并为用催化剂和 H 2替代化学计量还原剂铺平了道路.
