The Synthetic Process Optimization Of Mitiglinide

Mitiglinide belongs to the non-sulfonylurea drug which can stimulate release ofinsulin, it shows much advantages such as taking the medicine flexibly,safely,workrapidly,intensively and short-acting． Aimed at the questions that old methodssynthesizing Mitiglinide are costly, low efficiency and operated complexity, wedesigned a new route and defined the the optimal reacting process by referring to theold methods, considering the mechanisms and important factors of each steps, andexploring reacting conditions and operating process．Firstly this paper introduced the structure, characters, mechanism of drug actionand the previous preparation methods of Mitiglinide. And then, we improved theprevious routes to create a new one according to many references. Besides, this articleconducted a series of experiments to studied the reacting conditions and the factorsaffected the yield and achieved the optimized process of the route. Depending on thecurrent research situation, we determine the research direction: The synthetic researchand process optimization of Mitiglinide.In the experiment part, the target product was obtained starting frombenzaldehyde and diethyl succinate, via six-step reactions including Stobbecondensation, olefinic bond hydrogenation, resolution of enantiomers, amide bondhydrolyzation, ester bond hydrolyzation and salt formation. Through verifying themelting point,1H-NMR, and molecular rotation, and the analysis of the HPLCchromatography, the compound structure was determined. Experimental results showthat,the yield is up to14.01%after optimization. This new method has simpleoperation，inexpensive raw materials and efficient yield compare to other synthesisroutes, which is availability applied to factory production to bring large economicbenefits for the society.