The invention relates to a method for preparing tetraene acetate and derivatives thereof. The method comprises the steps of obtaining a compound II through etherification reaction of a compound I and an etherification agent in the
atmosphere of protective gases, obtaining a compound III through
addition reaction of the compound II and a
reagent A under the action of strong base and
hydrolysis and
elimination reaction of the compound II and the
reagent A in the presence of an acid solution, obtaining a compound IV through
substitution reaction and
rearrangement reaction of the compound III and acetate, and conducting 1 position
dehydrogenation and 2 position
dehydrogenation on the compound IV to obtain the tetraene acetate and derivatives thereof. According to the method, the compound I is taken as the
raw material and subjected to carbonyl etherification, addition,
hydrolysis,
elimination, rearrangement and
dehydrogenation reaction to obtain the product, the
raw material compound I is easy to obtain, cost is low, no
precious metal is needed during preparation,
reaction conditions are easy to control, operation is convenient, the method is suitable for large-scale industrial production, and the obtained tetraene acetate is an important intermediate for synthesis of
dexamethasone,
budesonide,
betamethasone and other steroidal drugs.