| 摘要 |
(a) Process for the preparation of penicillin and cephalosporin derivs. of formula (I) having respectively a 6 or 7-(alpha-( 4-R-2,3-dioxo-1-piperazino -carbonyl-amino)-4-R1-phenyl -acetamido) gp. and the cephalosporus having a 3-(1-methyl-tetrazol-5-yl thiomethyl gp.) by (a) reaction of a 6- or 7-(alpha-amino-4-R1-phenyl acetamido)-penicillin or cephalosporin (V) with phosgene or trichloromethyl chlorocarbonate to yield novel intermediates (X), (XI) or (XII) where the alpha amino is replaced by -NH-CO-Cl (X) -N=C=O (XI) or the lactam deriv. (XI); (b) reaction of the intermediates with trimethylchlorosilane activated derivs. of 1-R-2,3-dioxo-piperazine of formula (XIII) to form the cpds. (I). (Where R is H or 1-4C alkyl; R1 is H or hydroxy; M is H, an alkali metal atom e.g. K or Na or a quaternary ammonium gp. (having 1-4C alkyl gps.). Z is gp (Z). (I) are known antibiotics (described in BE-828629, FR application 75.14159 and JP kokai 52-106883) which have a broad spectram of activity against gram-negative and gram-positive bacteria Known preparations of (I) use 2,3-dioxo-piperazinocarbonyl chlorides which are difficult and costly to prepare and require several purification stages. The present process overcomes many of these problems. |
