Abstract: Provided is a method of preparation of (1R, 3S)-3-amino-1-cyclopentanol, the method including: contacting N-acylhydroxyamine and cyclopentadiene for an asymmetric cycloaddition, to yield a first intermediate I; hydrogenating the first intermediate I to yield a second intermediate II; hydrolyzing, ammonolyzing, hydrazinolyzing, or alcoholyzing an amido bond of the second intermediate II to yield a third intermediate III; and hydrogenating the third intermediate III to yield (1R, 3S)-3-amino-1-cyclopentanol.