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TitleA process for the selective synthesis of one enantiomer of venlafaxine via a novel approach
Knowhow is available forA novel approach towards total synthesis of (-)-venlafaxine with a short process for asymmetric synthesis of venlafaxine, wherein one enantiomer is obtained in improved yields and in high enantiomeric purity, circumventing the need for resolution
SummaryAPPLICATION:
- Acute treatment of major depressive disorder, generalized anxiety disorder
SUMMARY:
Venlafaxine is one of the most prescribed nontricyclic antidepressants. It has a well documented efficacy and safety for clinical use, with a reduced or completely diminished cardiovascular or anticholinergic liability. Venlafaxine is marketed in racemic form, although both R & S enantiomers show different bio activities i.e. S-enantiomer is a selective serotonin reuptake inhibitor, while R enantiomer is more selective towards norepinephrine transporter. Also, it has either no or has little activity on a variety of neuroreceptors. This invention fills the need for a synthetic process for the asymmetric total synthesis of either R or S venlafaxine using environment friendly reagents and ambient reaction conditions in the most concise manner possible so as to minimize the reaction steps in its synthesis
Advantages- Use of cheap and easily available raw materials
- Use of cost effective and environmentally friendly reaction conditions
- Avoidance of expensive catalysts
- Avoidance of additional steps involving resolution of enantiomers
- Improved overall yields with Enantiomeric purity >99%
- Strategy of asymmetric synthesis can be extended to the synthesis of both enantiomers
- Derivatives of venlafaxine can be prepared in the same manner


Knowhow is listed under following categories

Knowhow from
CSIR-NCL, Pune
Scientific/ engineering subject areas Chemical sciences & engineering
Investor interest categories Biotechnology/ Biomedical/ Health Technologies
Industries Pharmaceuticals, Bulk Drugs, Formulations ;