Alkylation of L-cysteine (I) with cyclopentylmethyl methanesulfonate (II) produced the cysteine thioether (III). A tert-butoxycarbonyl group was subsequently introduced into the amino group of (III) by using di-tert-butyl dicarbonate and NaOH. The resultant N-Boc-cysteine thioether (V) was finally coupled with p-methoxybenzylamine (VI) by means of EDC and HOBt to furnish the corresponding amide.