The invention relates to a method for preparing (1R,3S,4S)-N-tert-butyloxycarbonyl-2-azabicyclo[2,2,1]
heptane-3-
carboxylic acid (formula V), wherein the formula V is defined in the instruction. The method comprises: dissolving glyoxylate in a
solvent, cooling to a temperature of -10-0 DEG C, adding a
dewatering agent and (R)-phenyl
ethylamine, and at unit time intervals, sequentially adding an
alcohol solvent, an additive,
cyclopentadiene and
palladium carbon to carry out
catalytic hydrogenation and adding an inorganic alkali
aqueous solution and Boc anhydride to carry out a reaction. Compared with the method in the prior art, the method of the present invention has the following significant advantages that: the reaction operation is simple, the multi-step reaction is changed into the one-pot method, the production period is shortened, the separation purification is simple, the single configuration target product can be obtained only requiring the recrystallization, the yield is high, the reaction is efficient, the
atom economy is reflected, -78 DEG C and other harsh
reaction conditions are abandoned, and the method is expected to be used in
mass production.