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.