The invention discloses a 3-
trifluoromethyl-2,5-diazabicyclo[2.2.1]
heptane derivant and a preparation method thereof, mainly aiming to solve the technical problems that
bridged compounds with structure of 2,5-diazabicyclo[2.2.1]
heptane are restrained in extension of a space structure, and the compounds have poor water
solubility. The chemical
structural formula is as follows in the specification, wherein X is NR1 or O, R1 is a functional group or amino-substituted protective group, and is selected from one of H, C1-10 linear-chain or
substituent-side-chain-containing
alkyl, benzyl, 2,4-dimethoxybenzyl, 4-methoxybenzyl, tertiarybutoxy carbonyl,
carboxybenzyl, alkylacyl, aroyl, alkylsulfonyl or
aryl sulfonyl, and R2 is a functional group or amino-substituted protective group, and is selected from one of H, C1-10 linear-chain or
substituent-side-chain-containing
alkyl, benzyl, 2,4-dimethoxybenzyl, 4-methoxybenzyl,
carboxybenzyl, alkylacyl, aroyl, alkylsulfonyl or
aryl sulfonyl.