Abstract The synthesis of some 4-hydroxy-(or amino)-ethyl-amino butyrophenones or butyrothienones is described. The inter-conversion of these compounds to the corresponding 5-aryl-4-oxa-1-azabicyclo [3, 3, 0] octanes is presented. The title compounds demonstrated good antiinflammatory activity in the adjuvant induced disease model. They also possessed antinociceptive, immunomodulating and antioxidant activity, properties ...