cas 22316-47-8, CLOBAZAM | Articles data

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Method for industrially producing clobazam
The invention discloses a method for industrially producing clobazam, and belongs to the technical field of medicine synthesis. According to the method, 5-chloro-2-nitrobenzidine is used as a raw material, and a clobazam bulk drug is prepared through processes of acylation, reduction ring closing, methylation and refining. According to the invention, the problems that reagents with high toxicity are used in the prior art, the pollution is serious, and potential safety hazards exist in the pressurized hydrogenation reaction are solved, the production cost is reduced, and the product quality and economic benefits are improved.
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(2021/05/01)

Preparation method of clobazam
The invention provides a preparation method of clobazam. The preparation method comprises the following steps: (1), using 2-nitro-5-chlorodiphenylamine and ethyl malonyl chloride as raw materials, performing a reflow reaction in an organic solvent, after the reaction, decompressing the organic solvent in the reaction system, then performing evaporation to dryness, and adding a refining solvent for refining treatment so as to obtain a compound as shown in a formula II; (2), performing zinc powder reduction on the compound as shown in the formula II, and performing ammonolysis cyclization so as to obtain a compound as shown in a formula III; (3) enabling the compound as shown in the formula III to react with methyl iodide in an alkaline alcohol solution so as to obtain the clobazam, wherein alkali is one or more of sodium hydroxide, lithium hydroxide and potassium hydroxide. The clobazam prepared by the method is few in impurities and high in purity.
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(2017/07/23)

PROCESS FOR PREPARING CLOBAZAM USING NOVEL INTERMEDIATES
Processes for preparation of 7-chloro-1-methyl-5-phenyl-1,5-dihydro- benzo[b][1,4]diazepine-2,4-dione (Clobazam) are provided. The present invention also relates to the novel intermediates and its use in preparation of clobazam.
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(2016/12/22)

Method being suitable for industrially producing clobazam
The invention discloses a method of industrially producing clobazam and belongs to the technical field of medicine synthesis. With 5-chloro-2-nitrobenzidine as an initial raw material, the method includes the steps of reduction with a nano heavy metal granular catalyst, catalytic condensation with Lewis acid, methylation, and purification to prepare the clobazam that satisfies clinical medicinal requirement. The method solves the problems of heavy toxicity and serious pollution in the prior art, is beneficial to labor protection and reduces production cost, and improves product quality and economic benefit.
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(2017/04/08)

AN IMPROVED PROCESS FOR THE PREPARATION OF CLOBAZAM AND ITS INTERMEDIATE
The present invention provides an improved process for the preparation of 8-chloro-1-phenyl- 1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione (hereafter referred to as the compound (IV)), which is useful as a key intermediate for the synthesis of Clobazam (referred to as the compound (I)) 7-chloro-1-methyl-5-phenyl-1H-benzo[b][1,4]diazepine-2,4(3H,5H)-dione. The process of the present invention further involves transformation of the compound (IV) into Clobazam (I), comprising (a) reacting the compound (II) (as described herein) with monoalkyl malonate in the presence of a coupling agent to obtain the compound (III) (as described herein); followed by the cyclization using a base; (b) reacting the compound-IV (as described herein) obtained from step (a) with methylating agent. The process of the present invention involves formation of novel intermediates methyl 3-((4- chloro-2-(phenylamino)phenyl)amino)-3-oxopropanoate (IlIa) and 3-((4-chloro-2- (phenylamino)phenyl)amino)-3-oxopropanoic acid (V).
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Page/Page column 10; 20

(2016/10/11)

DERIVATIVES OF 1-PHENYL-1,5-DIHYDRO-BENZO[B] [1.4]DIAZEPINE-2.4-DIONE AS INHIBITORS OF HIV REPLICATION
Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.
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(2011/09/19)

Discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly
The discovery of a 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione series of inhibitors of HIV-1 capsid assembly is described. Synthesis of analogs of the 1,5-dihydrobenzo[b][1,4]diazepine-2,4-dione hit established structure-activity relationships. Replacement of the enamine functionality of the hit series with either an imidazole or a pyrazole ring led to compounds that inhibited both capsid assembly and reverse transcriptase. Optimization of the bicyclic benzodiazepine scaffold to include a 3-phenyl substituent led to lead compound 48, a pure capsid assembly inhibitor with improved antiviral activity.
Fader, Lee D.,Bethell, Richard,Bonneau, Pierre,B?s, Michael,Bousquet, Yves,Cordingley, Michael G.,Coulombe, René,Deroy, Patrick,Faucher, Anne-Marie,Gagnon, Alexandre,Goudreau, Nathalie,Grand-Ma?tre, Chantal,Guse, Ingrid,Hucke, Oliver,Kawai, Stephen H.,Lacoste, Jean-Eric,Landry, Serge,Lemke, Christopher T.,Malenfant, Eric,Mason, Stephen,Morin, Sébastien,O'Meara, Jeff,Simoneau, Bruno,Titolo, Steve,Yoakim, Christiane
p. 398 - 404
(2011/03/17)

1,5-Benzodiazepine-2,4-diones
This invention relates to substituted 1,5-benzodiazepines having the formula SPC1 Wherein R1 and R2 are hydrogen or substituents, R3 is hydrogen or substituents, R4 is methyl or aryl group, As well as the process of producing the same. The compounds of the invention are tranquillizing analgesic, antipyretic and anti-inflammatory agents.
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(2008/06/13)

Benzodiazepines with psychotropic activity. 3. N-aryl- and N-heteroaryl-1H-1,5-benzodiazepine-2,4-(3H,5H)-diones
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Weber,Bauer,Hauptmann
p. 128 - 138
(2007/10/09)

Chemical Properties

Melting Point: 162-164°C
Boiling Point: 643.8°Cat760mmHg
Flash Point:343.2°C
Density: 1.335g/cm³
Solubility:Slightly soluble in water, freely soluble in methylene chloride, sparingly soluble in alcohol.
Storage Temp.:2-8°C
Vapor Pressure: 1.82E-16mmHg at 25°C
Refractive Index: 1.5200 (estimate)
PKA: 8.59±0.20(Predicted)
PSA: 40.62000
LogP: 3.50120

This product is a nationally controlled contraband, and the Lookchem platform doesn't provide relevant sales information.

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22316-47-8

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Chemical Properties

Melting Point: 162-164°C

Boiling Point: 643.8°Cat760mmHg

Flash Point:343.2°C

Density: 1.335g/cm³

Solubility:Slightly soluble in water, freely soluble in methylene chloride, sparingly soluble in alcohol.

Storage Temp.:2-8°C

Vapor Pressure: 1.82E-16mmHg at 25°C

Refractive Index: 1.5200 (estimate)

PKA: 8.59±0.20(Predicted)

PSA: 40.62000

LogP: 3.50120

Article Database

22316-47-8

Articles about 22316-47-8Total 9 be found

More Articles about upstream products of 22316-47-8

More Articles about downstream products of 22316-47-8

Chemical Properties

Melting Point: 162-164°C

Boiling Point: 643.8°Cat760mmHg

Flash Point:343.2°C

Density: 1.335g/cm3

Solubility:Slightly soluble in water, freely soluble in methylene chloride, sparingly soluble in alcohol.

Storage Temp.:2-8°C

Vapor Pressure: 1.82E-16mmHg at 25°C

Refractive Index: 1.5200 (estimate)

PKA: 8.59±0.20(Predicted)

PSA: 40.62000

LogP: 3.50120

Density: 1.335g/cm³