Cyclohexylalanine benzyl ester (I) is acylated by 4-morpholinecarbonyl chloride (II) to furnish the urea derivative (III). The benzyl ester group of (III) is then removed by transfer hydrogenolysis, yielding N-(4-morpholinecarbonyl)-L-cyclohexylalanine (IV).

N-Boc-O-Benzyl-L-serine (V) is treated with ammonium hydroxide and EDC/HOBt to afford the corresponding amide (VI). Subsequent acidic cleavage of the N-Boc group of (VI) provides O-benzyl-L-serinamide (VII). Then, coupling between cyclohexylalanine derivative (IV) and serinamide (VII) in the presence of EDC/HOBt furnishes the dipeptide derivative (VIII). Finally, dehydration of the terminal amide function of (VIII) by means of cyanuric chloride leads to the target nitrile.