PRODUCTION OF BETA-THIOLACTAM DERIVATIVE

摘要

PURPOSE: To simply and efficiently obtain aβ-thioloctam derivative useful as a physiologically active substance such as a penicillin-like antibiotic and as its synthetic intermediate by reacting dihydrofuran with an isothiocyanic acid ester which are easily available materials. CONSTITUTION: (A) An isothiocyanic acid ester of the formula: R-NCS (R is an alkyl, an aryl) and (B) 2,3-dihydrofuran preferably in a large excessive amount are subjected to an addition-cyclization reaction preferably under >=2000 atmospheric pressure (especially 2000-10000 atmospheric pressure) at 0-200 deg.C (especially 20-150 deg.C) usually for 1-50hrs. The reaction solvent includes an aliphatic hydrocarbon solvent, an alicyclic hydrocarbon solvent and an aromatic hydrocarbon solvent.