The invention discloses a preparation method of 3-methylol
cefazolin. The preparation method comprises the following steps of dropwise adding a 7-ACA solution to a 1H-
tetrazole-1-
acetic acid anhydridemixing solution, performing a
condensation reaction, after the reaction, adjusting pH
phase splitting, then adding
purified water, performing
phase splitting, combining water phases, then adding an
organic solvent for
phase splitting, and performing concentration to obtain a primary
purified water phase and a secondary
purified water phase; and after adjusting pH of the secondary purified water phase, adding
cephalosporin-C deacetylase, then adding a dispersing agent to the filtered water phase, then reducing the temperature, performing
filtration after
crystal formation, performing washing,and performing
drying until the
moisture is smaller than 1.0%. According to the preparation method disclosed by the invention, a traditional strong
basic hydrolysis technology is substituted, waste
water discharge can be reduced by 80%, the
cephalosporin-C deacetylase after enzymolysis can be in cyclic utilization,
solvent remains are smaller than 5%, the concentration weight
reduction ratio is 2%-5%, the influence of various solvents on the enzymatic activity of the
cephalosporin-C deacetylase is thoroughly eliminated, the consumption of enzymes and the activity of the enzymes being utilizedonce again are guaranteed, the cost is reduced, the reaction condition is mild, the conversion rate of products is as high as 90% or above, the purity of the products is not less than 98%, and subsequent structure elucidation and pharmacological research are facilitated.