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从各种3-氨基吡唑类和3-氯甲基头孢菌素衍生物,合成了如结构式Ⅰ所示的新头孢菌素类。广泛研究涉及绿脓杆菌的构效关系后,表明7β-[(Z)-2-(5-氨基-1,2,4-噻二唑-3)2-(1-羧基-1-甲基乙氧亚氨基)乙酰胺基-3-[3-氨基-2(2-羟乙基)-吡唑烷]甲基-3-头孢烯-4-羧酸盐——FK518(X=N,R_t=CH_3,R_2=N,R_3=(CH_2)_2OH)是一种行的非肠道应用,而对假单胞菌属具有效抗菌活性的头孢烯抗生素。已经从两二腈开发了相应于FK518中的7-酰基部分的二羧酸的有效合成。
From various 3-aminopyrazoles and 3-chloromethylcephalosporin derivatives, new cephalosporins of the formula I have been synthesized. Extensive studies on the structure-activity relationship of Pseudomonas aeruginosa have shown that 7β - [(Z) -2- (5-amino-1,2,4-thiadiazol-3) 2- Ethoxyimino) acetamido-3- [3-amino-2 (2-hydroxyethyl) -pyrazolidine] methyl-3-cephem-4- carboxylate - FK518 (X = R_t = CH_3, R_2 = N, R_3 = (CH_2) _2OH) is a parenteral use of cephalosporin antibiotics that have potent antibacterial activity against Pseudomonas. Efficient synthesis of dicarboxylic acids corresponding to the 7-acyl moiety in FK518 has been developed from dinalide.