| 摘要 |
PURPOSE:To obtain a 3-[(1R)-hydroxyethyl]azetidin-2-one derivative in high efficiency, by reacting the corresponding 3-[(1S)-hydroxyethyl]azetin-2-one derivative with trifluorodiethylaminosulfuric acid. CONSTITUTION:The objective (3R,4R)-4-[3-(4-nitrobenzyloxycarbonyl)-3-diazo-2- oxopropan--1-yl]-3-[(1R)-fluoroethyl]azetidin-2-one of formula II useful as an intermediate for a fluorine-containing carbepenem antibiotic substance is produced in high efficiency with an economical process, by reacting 1mol of 3-[(1S)- hydroxyethyl]azetidinone with 1-5mol, preferably 1-2mol of trifluorodiethylaminosulfuric acid in an inert organic solvent such as halogenated hydrocarbon, ether, etc., especially in methylene chloride, preferably at -80-0 deg.C. |
