Salenco (iii) Chiral Catalysts And Fluoxetine Enantiomer Intermediates Of Asymmetric Synthesis

Fluoxetine is a potent and selective inhibitor of neural serotonin-reuptake. It is effective not only as an antidepression, but also for treatment of anxiety, alcoholism, chronic pain, and eating disorder such as obesity and bulimia. It is very popular on market because of its effectivity and less side-effects. Because the individual enantiomers display different pharmacological activities and different metabolic behaviour, the preparation of the enantiomers of the drugs has attracted considerable attention. Resolution, enzymatic catalysts, chemical catalysts are all the effective and convenient approaches for preparing enantiomers of Fluoxetine. In our experiment, we attempt to apply chiral (Salen)Co(III)-catalyzed Hydrolytic kinetic resolution of racemic terminal epoxides to the syntheses of R- phenyloxiran of the important intermediate of preparing enantiomers of Fluoxetine .1. Basing on all kinds of literature, we worked out a new way of synthesis of fluoxetine which has not been used home and abroad, applying chiral (Salen)Co(III)-catalyzed Hydrolytic kinetic resolution of racemic terminal epoxides to the syntheses of R- phenyloxiran of the important intermediate of preparing enantiomers of Fluoxetine .2. For the synthesis and resolution of (±)-1,2-diphenylethanediamine,we gained the target product by three steps using benzaldehyde, a low-cost and easy-to-get chemical, as one of the original materials. During preparing all staples, we carefully compared and studied synthetical line and condition of reaction from temperature and time, and found the best way to obtain target product.3. During synthesis of chiral (Salen) Co(III)-catalyzed , we found the best way to prepare 2- butyl-4-methyl phenol by comparing all other ways and got the best reactive temperature and proportion of the involved materials. In the follow-up experiment of reactions, we made further exploration in terms of reactive temperature and time.4. In order to get R-phenyloxiran, we made full use of Chiral (Salen) Co-...