186694-45-1Relevant articles and documents
Synthesis method of high-purity stable crystal form of escilitalopine acetate
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Paragraph 0032-0035, (2022/03/18)
The present invention discloses a high-purity method for the synthesis of escitazepine acetate and a novel stable crystal form thereof. The preparation method disclosed in the present invention is achieved by the following steps: 10-methoxyiminopyrene as the starting material, the starting material is dissolved in acetone and deprotected to form 10-carbonyliminocarbenzene; the use of dichloromethane, borane dimethyl sulfide, (R)-2-methyl -CBS- oxazoleboran asymmetrical reduction to generate (10S)-10-hydroxyiminopyrene; (10S)-10-hydroxyiminostilbeneylated into esters, amidated with chlorosulfonyl isocyanate, To obtain escilitalopine acetate and a stable new crystal form. The preparation method provided by the present invention is simple synthesis process, few reaction steps, less pollution, raw materials are readily available and inexpensive, the final product is easy to purify and separate and the crystal form is stable, and the industrial application prospects are broad.
Recrystallization purification process for precursor reactant of asymmetric catalytic hydrogenation reaction
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Paragraph 0027; 0028; 0029; 0032-0038, (2018/12/13)
The invention provides a recrystallization purification device for a precursor reactant prepared from Eslicarbazepine and a derivative thereof. The device is characterized in that a recrystallizationpurification process and a recrystallization purification device are used, unreacted raw materials, byproducts and impurities in the precursor reactant are removed, toxicity of a chiral catalyst is eliminated, the conversion rate of the chiral catalyst is greatly increased, the yield of asymmetric hydrogenation is effectively increased, high production efficiency is achieved, and the cost performance of on-scale production of Eslicarbazepine and the derivative thereof is effectively increased.
Brain-targeting eslicarbazepine ester prodrug and application thereof
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, (2017/08/28)
The invention relates to an eslicarbazepine ester prodrug and an application thereof, wherein the prodrug is a compound represented by the formula (I) or optical isomers or physiologically acceptable salts of the compound represented by the formula (I), wherein R represents a lipophilic substituent. The compound represented by the formula (I) is the eslicarbazepine ester prodrug containing the lipophilic substituent, is converted into eslicarbazepine through metabolism in vivo to play pharmacological effects, and can be applied in preparation of drugs for treatment, prevention or adjuvant treatment of central nervous system diseases, such as epilepsy and the like.