| abstract |
The invention discloses a preparation method of Kebomei. Compound 1 and bis-dimethylaminomethane are heated and reacted in a mixed solvent of acetic acid and trifluoroacetic acid to form compound 2; acetic anhydride is added to the obtained reaction solution of compound 2 The heating reaction is completed to generate compound 3; compound 3 is dissolved in ethyl acetate and heated, catalyzed by Pd/C, and reduced with hydrogen to obtain compound 4; compound 4 and glycine are dissolved in a solvent, and compound 5 is obtained by heating under the action of an organic base. One or more of dioxane, ethylene glycol methyl ether, toluene, acetonitrile, and n-propanol, and the organic base is triethylamine, 1,8-diazabicycloundec-7-ene , N, N-diisopropylethylamine, one or more of N-methylmorpholine, pyridine, ethylenediamine; this preparation method is shorter than the existing route reaction time, and the reaction temperature is low, and the equipment conditions The requirement is not high, the purity of the crude product is high, it is suitable for large-scale industrial production, and the industrialization prospect is good. |