927-63-9Relevant articles and documents
A process for preparing pirazole carbaldehyde compounds
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Paragraph 0069-0077, (2018/02/24)
The present invention relates to a method for preparing pirazole carbaldehyde compounds and, more specifically, to a novel method for preparing 3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carbaldehyde and 3-(trifluoromethyl)-1-methyl-1-H-pyrazole-4-carbaldehyde which are useful as intermediates for producing pyrazole carboxanilide disinfectants such as isopyrazam, sedaxane, bixafen, etc. According to the present invention, production costs of pyrazole carboxanilide disinfectants can be reduced.COPYRIGHT KIPO 2017
Red-fluorescent argininamide-type NPY Y1 receptor antagonists as pharmacological tools
Keller, Max,Erdmann, Daniela,Pop, Nathalie,Pluym, Nikola,Teng, Shangjun,Bernhardt, Günther,Buschauer, Armin
scheme or table, p. 2859 - 2878 (2011/06/22)
Fluorescently labelled NPY Y1 receptor (Y1R) ligands were synthesized by connecting pyrylium and cyanine dyes with the argininamide-type Y1R antagonist core structure by linkers, covering a wide variety in length and chemical nature, attached to the guanidine group. The most promising fluorescent probes had Y1R affinities (radioligand binding) and antagonistic activities (calcium assay) in the one- to two-digit nanomolar range. These compounds turned out to be stable under assay conditions and to be appropriate for the detection of Y1Rs by confocal microscopy in live cells. To improve the signal-to-noise ratio by shifting the emission into the near infrared, a new benzothiazolium-type fluorescent cyanine dye (UR-DE99) was synthesized and attached to the parent antagonist via a carbamoyl linker yielding UR-MK131, a highly potent fluorescent Y1R probe, which was also successfully applied in flow cytometry.
Computer aided benzothiazole derivatives. Synthesis, structure and biological study of new push-pull conjugated benzothiazolium salts
Buffa,Zahradnik,Foltinova
, p. 331 - 336 (2007/10/03)
As the conjugation is assumed to enhance the biological activity of push-pull type benzothiazolium salts, new compounds with extended conjugated bridge between benzothiazolium and phenyl ring were designed and synthesized. The compounds have been tested against the model microorganism Euglena gracilis as well as 6 microorganisms including Gram-positive and Gram-negative bacteria , a yeast and a mould. In accordance with predictions, the prepared compounds showed enhanced activity against Euglena and Gram-positive bacteria and some of them also interesting fungicidal and fungistatic activity.
1-Acceptor Substituted Vinamidinium Salts: Stability and Reactivity
Bacher, Erwin,Gompper, Rudolf,Mertz, Ronald,Wagner, Hans-Ulrich
, p. 839 - 850 (2007/10/02)
1-Chloro- and 1,3-dichloro-vinamidinium salts react with potassium cyanide to afford 1-cyano- and 1,3-dicyano-vinamidinium salts.The former add nucleophiles at the C-3 position.MNDO calculations, competitive hydrolysis experiments and cyclic voltammetry reveal the following sequence of stabilities of vinamidinium salts: 1,3-(NMe2)2 > 1-NMe2 > 2-Aza > H > 2-(p-MeOC6H4) > 2-OMe > 2-Cl > 2-CN > 1,3-(SMe)2 > 1-Cl > 1-CO2Et > 2-NO2 > 1-CN > 1,3-(CN)2.Interestingly enough, reduction potentials show that 1,3-dicyanovinamidinium salt is more stable than a 1,3-dichlorovinamidinium salt, whereas a 1-chlorovinamidinium salt is more stable than a 1-cyanovinamidinium salt. - Keywords: Vinamidinium Salts, Hydrolysis, Cyclovoltammetry, MNDO Calculations
A Versatile New Synthesis of Quinolines and Related Fused Pyridines. Part 12. A General Synthesis of 2-Chloropyridines and 2-Pyridons
Meth-Cohn, Otto,Westwood, Keith T.
, p. 1173 - 1182 (2007/10/02)
The Vilsmeier formylation of tertiary and secondary enamides leads to 2-pyridons and 2-chloropyridines, respectively.The reaction appears to be quite general allowing substitution in the 1-, 3-, 5-, or 6-position or combinations of these.The major limitation arises with enamides which are unsymmetrically substituted on the double bond with alkyl groups, when mixtures can result.Attempts to introduce a 4-substituent by a variation of the Vilsmeier reagent had limited success.
A New Aromatic Annelation Reaction with Two Synthons, Enaminones and 3-Oxoglutarate. Studies on the β-Carbonyl Compounds Connected with β-Polyketides. VIII
Takeuchi, Naoki,Okada, Naomi,Tobinaga, Seisho
, p. 4355 - 4359 (2007/10/02)
Reactions of the enaminones 1 with dimethyl 3-oxoglutarate in the presence of KF-AcOH or AcONa-AcOH and 18-crown-6 gave the dimethyl 2-hydroxy-1,3-benzenedicarboxylates 3, providing a new aromatic annelation reaction.Keywords - enaminone; dimethyl 3-oxoglutarate; buffer catalysis; aromatic annelation; dimethyl 2-hydroxy-1,3-benzenedicarboxylate
A Versatile New Synthesis of Quinolines and Related Fused Pyridines. Part 5. The Synthesis of 2-Chloroquinoline-3-carbaldehydes
Meth-Cohn, Otto,Narine, Bramha,Tarnowski, Brian
, p. 1520 - 1530 (2007/10/02)
Acetanilides are converted into 2-chloroquinoline-3-carbaldehydes in good yield by the action of Vilsmeier's reagent in phosphoryl chloride solution.The reaction is shown to involve successive conversion of the acetanilide into an imidoyl chloride and then an N-(α-chlorovinyl)aniline.The latter enamine is diformylated at its β-position and subsequently cyclised to the chloroquinolinecarbaldehyde.The diformylated intermediates may be isolated in several cases and separately cyclised with polyphosphoric acid.
Studies on Peroxidized Lipids. I. Interaction of Malondialdehyde with Secondary Amines and Its Relevance to Nitrosamine Formation
Kikugawa, Kiyomi,Tsukuda, Koichi,Kurechi, Tsutao
, p. 3323 - 3331 (2007/10/02)
Malondialdehyde (MDA) reacted with secondary amines (dimethylamine, diethylamine, piperidine, pyrrolidine and morpholine) at 37 deg C under mild acidic or neutral conditions to yield β-dialkylaminoacroleins (1-5) of trans, s-trans conformation.The optimal pH of the reaction was 3-5, and the yields were 15-55percent in a 6 hr incubation.The acroleins (1-5) were unstable under acidic and alkaline conditions, and produced a pink color on reaction with 2-thiobarbituric acid. β-Dimethylaminoacrolein (1) could be readily nitrosated in the acidic pH range to produce N-nitrosodimethylamine, and the rate of nitrosamine formation from 1 at pH 5.0 was much higher than that from dimethylamine; this is consistent with earlier observations of the stimulating effect of MDA on nitrosamine formation.Keywords-malondialdehyde; β-dimethylaminoacrolein; β-diethylaminoacrolein; β-piperidinoacrolein; β-pyrrolidinoacrolein; β-morpholinoacrolein; β-dialkylaminoacrolein formation; N-nitrosodimethylamine formation; 2-thiobarbituric acid test.
