The invention relates to a synthesis method of a rilpivirine key intermediate, and belongs to the technical field of
pharmacy. The name of the intermediate is (E)-3-(4-amino-3, 5-dimethylphenyl)
acrylonitrile hydrochloride; the method comprises the following steps: 1, taking 2, 6-
dimethylaniline as a starting material, and carrying out
halogenation reaction and amino protection one-pot reaction to obtain an intermediate 1; step 2, carrying out
Heck reaction and post-treatment on the intermediate 1 and
acrylamide to prepare an intermediate 2; and step 3, carrying out
dehydration reaction on the
amide group of the intermediate 2 and carrying out one-time deprotection reaction on the amino group to finally obtain the required (E)-3-(4-amino-3, 5-dimethylphenyl)
acrylonitrile hydrochloride. According to the method, high temperature,
high pressure, toxic and harmful gas and the like are avoided in each step of operation, the method is very suitable for industrial production, and the technical scheme is high in yield and has great commercial application value.