- Preparation method of clobazam
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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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Paragraph 0027; 0028
(2017/07/23)
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- A 1,5-benzodiazepine derivatives zhuo Tong method for the preparation of (by machine translation)
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This invention relates to a kind of 1,5 the zhuo Tong[...] and method for preparing derivatives of nitrogen, characterized in that in order to replace the raw materials of dinitro compound is phthalic acid, with a substituted aniline reaction, the reaction with malonic acid monoester, then cyclization to obtain a target compound. The method step of this invention is simple, cheap material, easy to operate and achieve commercial, yield and purity are greatly improved. (by machine translation)
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- SYNTHESIS AND BIOLOGICAL EVALUATION OF 7-CHLORO-1-TRIDEUTERIOMETHYL-5-PHENYL-1H-1,5-BENZODIAZEPINE-2,4(3H,5H)-DIONE (CLOBAZAM-D3)
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Clobazam-d3 has been prepared by treatment of norclobazam sodium salt with trideuteriomethyl iodide.Clobazam-d3 has a pharmacological profile rather similar to that of clobazam.It differs by its longer duration of anti-epileptic action.Keywords - anti-epiliptic action / clobazam-d3
- Poupaert, Jacques H.,Guiot, Pierre,Jacqmin, Philippe,Dumont, Pierre
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p. 417 - 420
(2007/10/02)
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- 1,5-Benzodiazepine-2,4-diones
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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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