| 摘要 |
Penicillin and cephalosporanic derivs. of formula (I) [R1 = Ph, 4- hydroxyphenyl, 3,4-dihydroxyphenyl, 1-hydroxyethyl ; R2 = H or MeO; A = (CH3)2CH(COOH) or CH2C(CH2R3) = (COOH); R3 = 5-membened bicyclic contg. two or more than N and one S, or substd. with lower alkyl! was prepd. Thus, a soln. of 3.02g D(-)-α-(4-ethyl2,3-dioxo-1- piperazinylcarbonylamino) phenylacetate and 0.8 ml pyridine in 32 ml N,N-dimethylformamide was acylated with 2.96g 1,1'-(carbonyldioxy) dibenzotriazole at room temp. for 1h and later reacted with 2.27g 6- aminopenicillanic acid for 2h at room temp. The reaction mixt. was diluted with 1l H2O and adjusted to pH 2.0 with 2N HCl soln. to give 4.43g(I) H2O [R1 = phenyl, R2 = H, A = (CH3)2CH(COOH) .
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