The invention relates to the field of
chemistry or
medicinal chemistry, in particular to a synthesis method of isoxazoline anti-parasitic
drug lotirasodium. The synthesis method comprises the following steps: firstly, synthesizing an intermediate 1 (1, 2, 3-trichloro-5-(1-
trifluoromethyl-vinyl)
benzene); then synthesizing an intermediate 2 (5-bromo-4-methyl-2-thiophenecarboxime); the preparation method comprises the following steps: carrying out a 1, 3 dipolar
cycloaddition reaction on an intermediate 1 and an intermediate 2 in sequence to obtain an intermediate 3, carrying out a
Grignard reaction to obtain racemic acid, and finally carrying out chemical resolution and
amide condensation in sequence to obtain lotirasodium. According to the novel synthesis method of the isoxazoline anti-parasitic
drug lotirazine,
wittig reaction is adopted for the first time to obtain the intermediate 1, operation is simpler and more convenient, and
reaction conditions are mild. Besides, the synthesis method of the intermediate 2 is improved, so that the
reaction conditions are milder, the operation is simpler, the cost is greatly reduced on the basis of reported
reaction conditions, and the method is suitable for industrialization.