The Research On Preparation Processing Of Chiral Drug Of Organic Amine

In recent years, the clinical significance of chiral drugs caused the people’s extensive concern, The research and development of the chiral drugs made great progress and become the focus of new drug R&D.With further research done for pharmacological properties, differences have been recognized in physiological effect and metabolism of a pair of enantiomers of chiral drugs.Organic amine drugs are a large family of important compounds。There is a very widely used in clinic and play an important role in the development of medicine。It is necessary to research resolution for his class of drugs. obtained optically pure can highly devoted to improves the effect reducing its toxic side effects.Venlafaxine and sibutramine are typical organic amine drugs.This paper mainly deals with classic chemical separation method to split and improve its technology.Venlafaxine is a kind of antidepressants and have unique chemical structure and neuropharmacology effect. Which is suitable for various kinds of depression include associated with anxiety depression and generalized anxiety disorder.and has a good curative effect for Depression in patients with psychomotor retardation and vehement behavioral characteristics.The enantiomers of Venlafaxine were active, A single enantiomer drug can reduce side effects.The most common side effects have nausea sleepiness insomnia and headaches, etc. therefore, obtain chiral venlafaxine has a very large economic and social significance. The part of thesis maily researched the racemic resolution of venlafaxine.Through the resolution in the separation process of the solvent system, resolution agent, the main object than to explore dept studyof the use of tartaric acid derivatives resolute venlafaxine resolutionpreparation method and process conditions optimization. Among them,when using DTTA as resolving agent,the salt of non-enantiomer canbe facilely precipitated in THF and a small amount of water. Followe. and by recrystallization and dissociation, optically pure venlafaxine was obtained.Sibutramine is a function of the central nervous inhibitors。These maily researched the racemic of sibutramine at present, which is a drug for obesity functioning through central nerve system and is used in the racemic form in the clinic.Many studies have shown that the racemic form of drug delivery may lead to serious adverse reactions. Moreover, the enantiomers of sibutramine showed different effects in pharmacodynamic and pharmacokinetic.herefore, obtained optically pure sibutramine can highly devoted to the in-depth research of pharmacology, pharmacodynamics metabolism and the correct medicaton。This part mainly discusses resolution process, when using DMTA as resolving agent,the salt of non-enantiomer can be facilely precipitated in n-hexane, ratio of ethanol. Followed by recrystallization in isopropyl alcohol and dissociation,optically pure sibutramine was obtained.Through nuclear magnetic resonance (NMR), infrared, differential thermalgravimetric analysis(DSC/TGA) and other analytical testing methods,we study themechanism of chiral tartaric acid derivatives and Venlafaxine or substrate and Analyzed the difference between the two isomers.