The functionalization of the thiazepine system by 1,3-dipolar cycloadd
ition of benzonitriloxide to the C=N double bond of 1,5-benzothiazepin
e derivatives, is described. The configurational and conformational pr
operties of the l-5H-[1,2,4]oxadiazolo[5,4-d][1,5]benzothiazepines hav
e been determined by nmr spectroscopy assisted by NOE measurements.