Using inositol methyl ether as a raw material, it is converted into a diisopropylidene compound, catalytically oxidized to a ketone, stereoselectively epoxidized, hydrolyzed, the epoxy ring broken, two dimethyl ether bonds broken and disassembled, triisopropylated, selectively hydrolyzed and benzylated trans-isopropylidene, and then hydrolyzed again to the remaining two isopropylidene groups. Following selective benzoylation, methanesulfonation, epoxidation, acetylation, and elimination of the epoxy ring to form cyclohexenone, the acyl group is removed, selectively benzoylated, hydroxyazidated, and the azido group is reduced to an amino group and deprotected to obtain Valienamine.