Yin Hongxia
2006
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Journal
Journal of Jining Medical College
Abstract
Objective Study a practical total-synthetic method that is suitable to industrialization.Methods The S-(-)-timolol is prepared from a chiral synthon D-mannitol.The treatment of S-(-)-3-t-butylamino-1,2-propanediol with benzaldehyde afforded the oxazolidine derivative.S(-)-tomolol could be obtained from oxazolidine derivative by treatment with 3-chloro-4-morpholino-1,2,5-thiadiazole and t-BuOK in t-BuOH and hydrolization.At last give the target product.S-(-)-timolol.Results The synthetic route is determined and investigated after the analyzing and trying for the literal synthetic methods.Conclusion The synthetic technology of each step has been optimized,resulting in decreasing the cost and simplifying the operation procedures.