The invention discloses a synthesis method of octahydro-4A,8-
epoxy pyrido[4,3-C]
azepine-6(5H)-tert-
butyl formate. The synthesis method comprises the following steps: 1, reacting a compound 1 with a catalytic amount of
osmium tetroxide and a first oxidant to obtain a compound 2; 2, oxidizing an alcoholic hydroxyl group into an
aldehyde group by the compound 2 under the action of a second oxidant to obtain a compound 3; 3, subjecting the compound 3 and benzyl amine to reduction ammoniation in an
inert atmosphere under the action of a first
reducing agent to obtain a compound 4; 4, subjecting the compound 4 to
catalytic hydrogenation through a
palladium catalyst in the presence of Boc2O to obtain a compound 5; 5, reducing the compound 5 through a second
reducing agent to obtain a compound 6; and 6, carrying out
catalytic hydrogenation on the compound 6 under the action of a
palladium catalyst to obtain a compound 7. The method disclosed by the invention has the advantages of easily available raw materials, convenience in operation, safety in reaction, suitability for amplification, short
route, high total yield, suitability for industrial production and the like.