| 摘要 |
PURPOSE:To directly produce a synthetic intermediate for beta-lactam compound useful as an antibiotic substance at a low cost by using easily available safe trifluoromethanesulonate copper and a disulfide as starting materials and reacting with a beta-lactam compound. CONSTITUTION:The objective compound of formula I can be produced by using a beta-lactam of formula I [R1 is aryl, 1-10C straight or branched substituted or unsabstituted alkyl, allyl, aralkyl, alkenyl or alkynyl; R2 is silyl or formula R'R''R'''Si (R', R'' and R''' are 1-10C alkyl, etc.); R3 is H or amino-protecting group such as alkyl or aralkyl] as a raw material and reacting with a disulfide compound of formula II (R4 is aralkyl, aryl or 1-5C lower alkyl) and trifluoromethanesulfonate copper in the presence of a base, preferably in the presence of calcium carbonate, in a solvent (e.g. benzene) at -78 to +200 deg.C (especially 50-120 deg.C). |
