The invention relates to Omarlliptin, in particular to a novel method for preparing Istradafylline, and relates to a preparation method of Istradafylline, in particular to a preparation method of Istradafylline. The method comprises the following steps: carrying out
coupling reaction on a compound Ia and TMS
acetylene to obtain an intermediate Ib; carrying out bromination reaction on the intermediate Ic under the action of NBS (N-
bromosuccinimide) to obtain an intermediate Id; carrying out
substitution reaction on the intermediate Id and tert-
butyl carbamate under the action of
potassium tert-butoxide to obtain an intermediate Ie; reacting the intermediate Ie with
paraformaldehyde to obtain an intermediate If; carrying out
cycloaddition reaction on the intermediate If and the intermediate Ib to obtain a key intermediate Ig; carrying out asymmetric
catalytic hydrogenation reduction on the intermediate Ig to obtain an intermediate Ih; and removing a
protecting group from the intermediate Ih in a
hydrochloric acid and
ethyl acetate system to obtain a final product. The method is short in
route, simple and convenient to operate, mild in condition, high in reaction yield, environment-friendly and easy for industrial production, and dangerous and highly toxic products are prevented from being used and hazardous chemicals are supervised. # imgabs0 #