59467-64-0Relevant articles and documents
Preparation method of midazolam intermediate defluoro impurity
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Paragraph 0027; 0031, (2021/07/24)
The invention relates to the technical field of organic synthesis, and provides a preparation method of a midazolam intermediate defluoro impurity. The method comprises the following steps of: dissolving a midazolam intermediate in an organic solvent, adding Lewis acid and a reducing agent for reaction, performing extraction and chromatography on reaction liquid to obtain a crude defluoro impurity, and salifying the crude defluoro impurity with maleic acid to obtain the high-purity defluoro impurity. According to the synthesis method provided by the invention, the midazolam intermediate defluoro impurity can be obtained only through one-step reaction, and the synthesis method has a great promotion effect on optimization of production process parameters of midazolam, deep research on related substances of midazolam, improvement of the medication safety, reliability and stability of related preparations, and quality control in the production process of raw material medicines.
A nitrogen-containing seven-membered ring derivatives of industrial production method
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Paragraph 0089-0093, (2016/12/01)
The invention provides an industrial production method of a nitrogenous seven-member-ring derivative. The industrial production method is characterized in that the nitrogenous seven-member-ring derivative is generated from a compound A and a compound B which participate in a cyclization reaction under a condition of acid catalysis. The production method disclosed by the invention is simple, and is different from complex production modes and harsh production conditions in the prior art; a target product can be synthesized by one step; and compared with multi-step synthesis in the prior art, the industrial production method has the advantages that the yield is improved by 50% at least. In addition, by optimizing the production process and synthesis route, in the production process, the production method is less in side effect, convenient in post-treatment, mild in production condition, and suitable for an industrial production mode.
Imidazodiazepines and processes therefor
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, (2008/06/13)
Novel Imidazobenzodiazepines and their analogs are useful as anticonvulsants, muscle relaxant, anxiolytic and sedative agents. Preferred compounds of this class belong to the imidazo[1,5-a][1,4]diazepine series which may have a very wide variety of organic substituents. An especially preferred genus included within the purview of the invention encompasses a compound of the formula STR1 wherein R1 is hydrogen and lower alkyl preferably methyl; R3 and R5 are hydrogen; R4 is hydrogen, nitro and halogen, most preferably, chlorine, and in a most preferred embodiment when positioned on the fused benzo portion of the imidazobenzodiazepine is in the 8-position thereof, R6 is phenyl or halo, nitro, or lower alkyl-substituted phenyl, preferably, halo, with fluorine being the preferred halogen, the substituted fluoro being positioned in the 2-position of the phenyl moiety and R2 is hydrogen and lower alkyl.