102878-84-2

Usage

Uses

Quinoline derivative as antibacterial agents.

Upstream product

• 23261-58-7 quinoline-5-sulfonic acid 
• 3056-03-9 5-mercaptoquinoline 
• 611-34-7 5-Aminoquinoline 
• 60999-26-0 5,5'-bisquinolinyl disulfide 

Downstream Products

• 415913-05-2 quinoline-5-sulfonamide 
• 1155860-39-1 C₂₂H₂₁Cl₂N₃O₃S 
• 1428128-19-1 sodium 1-(5-chloro-2-((4-chloro-2-fluorobenzyl)oxy)benzyl)-1,2,3,4-tetrahydroquinoline-5-sulfonate 
• 23261-58-7 quinoline-5-sulfonic acid 
• 109869-21-8 5-benzoylmercapto-1-methyl-quinolinium; methyl sulfate 
• 110334-38-8 5-benzoylmercapto-1-methyl-quinolinium; iodide 
• 127133-87-3 thiobenzoic acid S-[5]quinolyl ester 

Relevant academic research and scientific papers

Synthesis, 15N NMR spectra and GIAO calculated data of the seven positional isomers of 15N-labeled N,N-dimethylsulfamoylquinoline

The one-step synthesis of positional isomers of N,N- dimethylsulfamoylquinoline are presented. Seven newly synthesized compounds have been characterized by elemental analyses, MS, 1H and 15N NMR spectral data. The long-range correlations between the ring protons and the endocyclic nitrogen atoms were observed in the gHMBC experiments. The spectral positions of the nitrogen atoms from the sulfonamide groups were drawn from the 1D spectra of the 15N-labeled sulfonamide isotopomers. Correlations between the experimentally determined chemical shifts and GIAO calculated isotropic shielding constants were found. The GIAO calculations were based on HF-, MP2-, and B3LYP-optimized geometries and were performed at the HF, BLYP, and B3LYP levels of theory.

Preparation method of genotoxic fasudil hydrochloride impurities

The invention relates to a preparation method of genotoxic fasudil hydrochloride impurities. The preparation method specifically comprises the following steps: preparing the fasudil hydrochloride impurities including methyl 5-isoquinolinesulfonate, ethyl 5-isoquinolinesulfonate, methyl 8-isoquinolinesulfonate, ethyl 8-isoquinolinesulfonate, methyl 5-quinolinesulfonate, ethyl 5-quinolinesulfonate,methyl 8-quinolinesulfonate and ethyl 8-quinolinesulfonate: firstly preparing isoquinolinesulfonyl chloride hydrochloride or quinolinesulfonyl chloride hydrochloride from isoquinoline sulfonic acid orquinoline sulfonic acid used as an initial raw material and thionyl chloride, and then reacting the isoquinolinesulfonyl chloride hydrochloride or quinolinesulfonyl chloride hydrochloride with methylalcohol and ethyl alcohol respectively to generate the corresponding fasudil hydrochloride methyl ester and ethyl ester impurities. The invention also provides a method for synthesizing the genotoxicfasudil hydrochloride impurityies with high purity to solve the problems of poor stability, easy rearrangement and easy decomposition of methyl quinolinesulfonate and ethyl ester.

EP1 RECEPTOR LIGANDS

The present invention belongs to the field of EP1 receptor ligands. More specifically it refers to compounds of general formula (I) having great affinity and selectivity for the EP1 receptor. The invention also refers to the process for their preparation, to their use as medicament for the treatment and/or prophylaxis of diseases or disorders mediated by the EP1 receptor as well as to pharmaceutical compositions comprising them.

From haloquinolines and halopyridines to quinoline- and pyridinesulfonyl chlorides and sulfonamides

The action of sodium methanethiolate (in boiling DMF) towards haloazines (i.e. chloro- or bromo-pyridines and quinolines) (1) (with halogen substituent in non-aza-activated position) causes sequentially halogen ipso-substitution to methylthioazines (2) and then S-demethylation to azinethiolates (3A), which were: i) subjected to S-methylation, ii) oxidized to diazinyl disulfides (4) and iii) oxidatively chlorinated to azinesulfonyl chlorides (5). α- and γ-pyridine- and quinolinesulfonyl chlorides (5a, 5c, 5d and 5f) were prepared by oxidative chlorination of respective disulfides (4) performed in conc. hydrochloric acid and characterized by 1H and 13C NMR spectra. All azinesulfonyl chlorides (5) were effectively converted to corresponding azinesulfonamides (6).

Identification and optimization of anthranilic sulfonamides as novel, selective cholecystokinin-2 receptor antagonists

A high throughput screening approach to the identification of selective cholecystokinin-2 receptor (CCK-2R) ligands resulted in the discovery of a novel series of antagonists, represented by 1-[2-[(2,1,3-benzothiadiazol-4- ylsulfonyl)amino]-5-chlorobenzoy

GLYT1 TRANSPORTER INHIBITORS

The invention provides a compound of formula (I): or a salt, solvate or a physiologically functional derivative thereof, wherein R1 to R10 are as defined in the specification and uses of such compounds. The compounds inhibit GlyT1 transporters and are useful in the treatment of certain neurological and neuropsychiatric disorders, including schizophrenia.