The condensation of 4-amino-1-benzylpiperidine (I) with 2,5-dimethoxytetrahydrofuran-3-carbaldehyde (II) under modified Paal-Knorr conditions produced the pyrrole derivative (III). Construction of the target oxazole ring was then achieved by cyclocondensation reaction of aldehyde (III) with tosylmethyl isocyanide in the presence of NaOMe.