51282-49-6

Usage

InChI:InChI=1/C8H6ClNO4/c1-14-8(11)6-4-5(9)2-3-7(6)10(12)13/h2-4H,1H3

Upstream product

• 67-56-1 methanol 
• 41994-44-9 5-chloro-2-nitrobenzoyl chloride 
• 2516-95-2 5-chloro-2-nitrobenzoic acid 
• 77-78-1 dimethyl sulfate 
• 2905-65-9 methyl 3-chlorobenzoate 
• 7697-37-2 nitric acid 
• 74-88-4 methyl iodide 
• 121-44-8 triethylamine 
• 79-22-1 methyl chloroformate 

Downstream Products

• 134050-75-2 methyl 5-(N-morpholinyl)-2-nitrobenzoate 
• 119198-42-4 methyl 5-(4-benzyl-1-piperazinyl)-2-nitrobenzoate 
• 60912-45-0 methyl 2-nitro-5-(2-nitrophenylthio)benzoate 
• 133446-90-9 methyl 4-<<3-(methoxycarbonyl)-4-nitrophenyl>thio>benzoate 
• 75355-02-1 2,5-di(phenylthio)benzoic acid 
• 5202-89-1 4-chlorobenzenesulfonyl chloride 
• 30541-56-1 adamantylidene-adamantane 
• 6628-86-0 5-chloro-2-nitrobenzaldehyde 
• 75355-01-0 methyl 2,5-di(2-nitrophenylthio)benzoate 
• 344779-31-3 5-chloroisatoic anhydride 
• 150683-30-0 tolvaptan 
• 160129-45-3 7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one 
• 247237-38-3 N-p-toluenesulfonyl-5-chloro-anthranilic acid methyl ester 
• 247237-83-8 1-(4-aminobenzoyl)-7-chloro-5-methoxy-2,3,4,5-tetrahydro-1H-1-benzazepine 

Relevant academic research and scientific papers

Preparation method of nitrobenzoate

The invention relates to the field of pesticides, and particularly discloses a preparation method of nitrobenzoate, wherein the structure of the nitrobenzoate is represented by a formula (2). The preparation method of the nitrobenzoate comprises the step that in the presence of a halogenated hydrocarbon organic solvent, a compound with a structure represented by the formula (1) makes contact withfuming nitric acid, fuming sulfuric acid and acetic anhydride, wherein in the formula (1) and the formula (2), X represents halogen, and R represents alkyl with the carbon atom number being 1-8. According to the method, the amount of waste acid can be reduced, and nitrobenzoate can be obtained at high yield.

Discovery of novel phenoxybenzamide analogues as Raf/HDAC dual inhibitors

Histone deacetylase (HDAC)inhibitors as an important epigenetic therapeutic strategy affect signaling networks and act synergistically with kinase inhibitors for the treatment of cancer. Herein we presented a series of novel phenoxybenzamide analogues with inhibition of Raf and HDAC. Among them, compound 10e showed potent antiproliferative activities against Hepg2 and MDA-MB-468 in cellular assays. This work may lay the foundation for developing novel dual Raf/HDAC inhibitors as potential anticancer therapeutics.

Tuning a robust system: N,O zinc guanidine catalysts for the ROP of lactide

Non-toxic, highly active and robust complexes are the holy grail as ideal green catalysts for the polymerisation of biorenewable and biodegradable polylactide. Four new zinc guanidine complexes [ZnCl2(TMG4NMe2asme)], [ZnCl2(TMG5Clasme)], [ZnCl2(TMG5Measme)] and [ZnCl2(TMG5NMe2asme)] with different electron-donating and electron-withdrawing groups on the ligand's aromatic backbone have been synthesised. Ligands are derived from low-cost commercially available compounds and have been converted by a three- or four-step synthesis process into the desired ligand in good yields. The compounds have been fully characterised and tested in the ROP of rac-LA under industrially relevant conditions. The complexes are based on the recently published structure [ZnCl2(TMGasme)] which has shown high activity in the polymerisation of lactide at 150 °C. Different substituents in the para-position of the guanidine moiety significantly increase the polymerisation rate whereas positioning substituents in the meta-position causes no change in the reaction rate. With molecular weights over 71000 g mol-1 being achievable, the best system produces polymers for multiple industrial applications and its polymerisation rate approaches that of Sn(Oct)2. The robust systems are able to polymerise non-purified lactide. The initiation of the polymerisation is suggested to occur due to impurities in the monomer.

PROCESS FOR PREPARING TOLVAPTAN INTERMEDIATES

The present invention provides a novel process for the preparation of 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one. The present invention also provides an improved process for the preparation of 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. The present invention further provides an improved process for the preparation of 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine.

Synthesis, characterization and evaluation of some 5-substituted 1,3,4-oxadiazole-2-thioesters as antifungal agents

A series of 5-substituted 1,3,4-oxadiazole-2-thioesters was synthesized by converting several substituted organic acids successively into the corresponding esters, hydrazides and 5-substituted 1,3,4-oxadiazole-2-thiols. Finally the target compounds: 5-substituted 1,3,4-oxadiazole-2-thioesters were obtained by refluxing 5-substituted 1,3,4-oxadiazole-2-thiols in the presence of acid chloride and potassium hydroxide. The structures of the synthesized compounds were established by physicochemical and spectroscopic methods. The synthesized compounds were evaluated for their in vitro antifungal activity. Some of the evaluated compounds possessed significant antifungal activity as compared to a terbinafine standard.

PROCESS FOR PREPARING TOLVAPTAN INTERMEDIATES

The present invention provides a novel process for the preparation of 7-chloro-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one. The present invention also provides an improved process for the preparation of 7-chloro-1-(2-methyl-4-nitrobenzoyl)-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine. The present invention further provides an improved process for the preparation of 7-chloro-1-[2-methyl-4-[(2-methylbenzoyl)amino]benzoyl]-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine.

Synthesis, characterization and antifungal activity of some new 5-substituted 1,3,4-oxadiazole-2-thiols

A series of 5-substituted 1,3,4-oxadiazol-2-thiols (3a-i) was synthesized by refluxing variably substituted organic acids (Ra-i) with methanol to the corresponding esters (1a-i). These esters were then converted to hydrazides (2a-i) by reaction with hydrazine hydrate in the presence of absolute ethanol which was followed by reaction with carbon disulfide and potassium hydroxide. Structure of the synthesized compounds was established by physicochemical and spectral data analysis. Synthesized compounds were subjected to antifungal activity. Antifungal activity was performed against Aspergillus flavus, Mucor species, Aspergillus niger and Aspergillus fumigates, with test compounds at a concentration of 200 μg/mL. Terbinafine was used as the standard drug.

Synthesis, characterization and antifungal activity of some 5-substituted 4-amino-1,2,4-triazole-3-thiols

A series of 5-substituted 4-amino-1,2,4-triazole-3-thiols (4a-i) was synthesized by refluxing substituted organic acids (a-i) with methanol to the corresponding esters (1a-i). These esters were then converted to hydrazides (2a-i) by reaction with hydrazine hydrate in the presence of absolute ethanol. The hydrazides were then converted to 5-substituted 1,3,4-oxadiazole-2-thiols (3a-i) by cyclization reaction with carbon disulfide and KOH which was followed by reaction with hydrazine hydrate in the presence of absolute ethanol. Structure of the synthesized compounds was established by physico-chemical and spectral data analysis. Synthesized compounds were subjected to antifungal activity. Antifungal activity analysis was performed against Aspergillus flavus, Mucor species, Aspergillus niger and Aspergillus fumigates, with test compounds at a concentration of 200 μg/mL. Terbinafine was used as the standard drug.

HOMOGENEOUS TIME RESOLVED FLUORESCENCE BASED TEST SYSTEM

The present invention concerns a fluorescence resonance energy transfer based high throughput test system to measure the formation of the HIV gp41 six-helix bundle. In a first embodiment the current invention relates to a homogeneous time resolved fluorescence-based test system comprising a first helical polypeptide consisting essentially of the sequence of IQN36 (SEQ ID NO:1); a second helical polypeptide consisting essentially of the sequence of C34 (SEQ ID NO: 2) wherein said IQN36 is labeled with a light emitting fluorophore and said C34 is labeled with an ultra-violet excitable fluorophore.

BIS-ARYL COMPOUNDS FOR USE AS MEDICAMENTS

There is provided compounds of formula I, wherein ring A, D1, D2a, D2b, D3, L1, Y1, L3 and Y3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful in the treatment of diseases in which inhibition of leukotriene C4 synthase is desired and/or required, and particularly in the treatment of a respiratory disorder and/or inflammation.