The invention relates to an efficient preparation method and application of optically pure beta-cyanone. The invention belongs to the technical field of
fine chemical synthesis. The invention aims to solve the technical problems of low yield, long reaction time, harsh
reaction conditions and unsuitability for industrial production of the existing method for preparing optically pure beta-cyanone through asymmetric conjugate cyanidation
addition reaction. According to the method, an alpha, beta-unsaturated carbonyl compound is taken as a substrate,
acetone cyanohydrin is taken as a
cyanogen source, and under the action of a cinchona alkali derivative, alkali and an additive, the optically pure beta-cyanoketone is prepared by heating in a
nitrogen atmosphere in one step without tedious operation. By screening cinchona
alkaloid derivatives, alkali, additives,
reaction temperature and reaction solvents and coordinating and controlling the optimal proportion of all the substances, side reactions are inhibited to the maximum extent, beta-cyanoketone is obtained with high
stereoselectivity and yield, and possibility is provided for industrial production of optically pure beta-cyanoketone. The method is mild in condition, simple in operation process, short in reaction time and
environmentally friendly,
acetone cyanohydrin serves as a
cyanogen source, substances such as highly toxic
sodium cyanide, TMSCN low in atom
utilization rate and high in price are replaced, the application range of a substrate is good, and the method can be widely applied to the fields of
biochemistry and
medicinal chemistry.