The acylation of 2-pyridylmethanol (I) with thioacetic acid (II) by means of Ph3P and DEAD in THF gives the corresponding thioacetate (III), which is condensed with 4-acetoxyazetidin-2-one (IV) by means of NaOH in methanol yielding 4-(2-pyridylmethylsulfanyl)azetidin-2-one (V). Finally, this compound is condensed with 1(R)-phenylethyl isocyanate (VI) by means of Et3N and DMAP in dichloromethane.