Boc-protected vigabatrin (II) was prepared from vigabatrin (I) by treatment with 2-(tert-butoxycarbonyloxyimino)-2-phenylacetonitrile. Coupling of the protected vigabatrin (II) with methyl nipecotate (III) in the presence of EDC and HOBt afforded the corresponding amide (IV). The Boc protecting group of (IV) was finally cleaved by treatment with trifluoroacetic acid.