| abstract |
The invention relates to a preparation method of bortezomib. The preparation method of bortezomib comprises the following steps of: (1) carrying out a condensation reaction on L-phenylalanine and pyrazine-2-formic acid to obtain N-(pyrazine-2-formyl)-L-phenylalanine; (2) carrying out condensation reaction on (R)-1-amino-3-methyl butane-1-boric acid hydrochloride and N-(pyrazine-2-formyl)-L- phenylalanine to obtain bortezomib. The preparation method of bortezomib has the advantages that (R)-1-amino-3-methyl butane-1-boric acid hydrochloride is taken as a reaction raw material, and R)-1-amino-3-methyl butane-1-boric acid hydrochloride is dropwise added to a reaction liquid at a low temperature, so that a side reaction is avoided; meanwhile, a step of removing a protecting group from boric acid is eliminated, so that a reaction period is shortened, production cost is reduced, and product loss in a protection removing step is reduced, and the yield and purity of the bortezomib product are increased. |