| 摘要 |
PURPOSE:To obtain a brominated beta-lactam compound with simple operation in high purity and yield by using a beta-lactam compound as a starting raw material, successively reacting with a sulfonic acid derivative, an amine and a bromination agent and hydrolyzing the reaction product. CONSTITUTION:This brominated beta-lactam compound of the formula IV or its keto-form tautomer can be produced by reacting the hydroxyl group of a beta- lactam compound of the formula I (Ar is aryl; R<1> is amino; R<2> is H or carboxyl- protecting group) with a reactive functional group derivative of a sulfonic acid of the formula HO-SO2-R<3> (R<3> is 1-18C hydrocarbon group), reacting the obtained beta-lactam compound of the formula II with a compound of the formula H-N(R<4>R<5>) [N(R<4>R<5>) is aminol, reacting the resultant beta-lactam compound of the formula III with a bromination agent and finally hydrolyzing the obtained brominated beta-lactam compound of the formula IV under acidic condition. The compound of the formula IV is an important intermediate easily convertible to a 3- hydroxycephalosporin intermediate which is a synthetic raw material for cefaclor, ceftibuten, etc. |
