专利号:WO-2025136150-A1 优先权日:2023-12-20 标 题:Method for producing dexmedetomidine and pharmaceutically acceptable salts thereof 发明人:ORECHOV DMITRII SERGEEVICH; VIOLIN BORIS VIKTOROVICH 权利人:OBSHESTVO S OGRANICHENNOI OTVETSTVENNOSTIU VIK ZDOROVE ZHIVOTNYKH 摘要:The invention relates to the field of pharmaceutical chemistry and describes a method for producing dexmedetomidine and pharmaceutically acceptable salts thereof. The invention solves the technical problem of developing an inexpensive dexmedetomidine synthesis method that produces minimal waste. The technical result consists in providing greater efficiency by increasing the degree of extraction of dexmedetomidine from a racemic mixture. This result is achieved by enriching medetomidine with an S-enantiomer in the early stages of synthesis, using an effective method for recovering 'chiral waste', as well as separated amine.
专利号:US-11718586-B2 优先权日:2019-11-08 标 题:Method for preparing dexmedetomidine 发明人:DIKER KHALID; GORINS GILLES; OZANNE-BEAUDENON AURÉLIE; GOLDSTEIN CORINNE 权利人:NORCHIM 摘要:The present invention relates to a method for preparing dexmedetomidine having the following formula (I): or a pharmaceutically acceptable salt and/or solvate thereof, comprising the following successive steps: a) asymmetric hydrogenation of a methylene derivative of the following formula (II): in order to obtain dexmedetomidine, and b) optionally salifying and/or solvating dexmedetomidine in order to obtain a pharmaceutically acceptable salt and/or solvate of dexmedetomidine, wherein the methylene derivative of formula (II) is prepared from a halide of the following formula (V), in which Hal 2 represents a halogen atom such as Br, and a cyanoimidazole of the following formula (VI). The present invention relates also to methods for preparing synthesis intermediates of dexmedetomidine from the halide of formula (V) and the cyanoimidazole of formula (VI), these synthesis intermediates being the methylene derivative of formula (II), an alcohol of the following formula (III), and a ketone of the following formula (IV).
专利号:CN-115108993-A 优先权日:2022-07-15 标 题 :A kind of chiral catalytic synthesis method of dexmedetomidine hydrochloride
专利号:CN-113800999-A 优先权日:2021-10-18 标题 :A kind of dexmedetomidine hydrochloride impurity and its synthesis method and application