The invention belongs to the technical field of
organic synthesis. The invention particularly relates to a preparation method of an
edoxaban intermediate. The method comprises the following steps: by taking 2, 5-dimethyl-4, 5, 6, 7-tetrahydrothiazole [5, 4-c]
pyridine (compound 1) as a
raw material, firstly carrying out oxidation reaction with an
oxidizing agent to obtain 5-methyl-4, 5, 6, 7-tetrahydrothiazole [5, 4-c]
pyridine-2-
formaldehyde (compound 2), then carrying out reaction with
chlorite to obtain 5-methyl-4, 5, 6, 7-tetrahydrothiazole [5, 4-c]
pyridine-2-
formic acid (compound 3), and finally, carrying out reaction on the 5-methyl-4, 5, 6, 7-tetrahydrothiazole [5, 4-c] pyridine-2-
formic acid (compound 3) to obtain 5-methyl-4, 5, 6, 7-tetrahydrothiazole [5, 4-c] pyridine-2-
formic acid (compound 3). And finally salifying in an organic solution of
hydrochloric acid to obtain the
edoxaban intermediate (compound 4). The method has the advantages of short reaction
route, cheap and easily available materials, mild
reaction conditions, high
atom economy, high product purity, product quality meeting subsequent requirements, and high yield. # imgabs0 #