33643-46-8Relevant articles and documents
Cycloalkyl-Diamines for the Treatment of Pain
-
Paragraph 0175-0180, (2021/02/26)
The invention is directed to a method of treatment for pain, the method comprising administering to a mammal in need of such treatment a therapeutically effective amount of a compound of formula I, or a pharmaceutically acceptable salt thereof.
Racemization method of ketamine and derivative or salt thereof
-
Paragraph 0113; 0114, (2021/02/20)
The invention discloses a racemization method of ketamine and a derivative or salt thereof. The racemization method comprises the following step: in a solvent, under the action of a catalyst and at the reaction temperature of 110-200 DEG C, carrying out a
Process Research and Impurity Control Strategy of Esketamine
Gao, Shenghua,Gao, Xuezhi,Yang, Zhezhou,Zhang, Fuli
, p. 555 - 566 (2020/05/19)
An improved synthesis of (S)-ketamine (esketamine) has been developed, which was cost-effective, and the undesired isomer could be recovered by racemization. Critical process parameters of each step were identified as well as the process-related impurities. The formation mechanisms and control strategies of most impurities were first discussed. Moreover, the (S)-ketamine tartrate is a dihydrate, which was disclosed for the first time. The practicable racemization catalyzed by aluminum chloride was carried out in quantitative yield with 99% purity. The ICH-grade quality (S)-ketamine hydrochloride was obtained in 51.1% overall yield (14.0% without racemization) by chiral resolution with three times recycling of the mother liquors. The robust process of esketamine could be industrially scalable.