A new synthesis of Cefepime.docVIP

 PAGE \* MERGEFORMAT 6 A new synthesis of Cefepime [ABSTRACT] GCLE as raw material, the first activation of C-3 halogenated seats are nucleophilic substitution reactions, ‘one pot’ off his C-7 Wei, C-2-bit, protected, and then to C-7 Wei condensation cephalosporin cefepime. The process target compounds derived from good quality, with a total yield of 36%, and the simple, easy-to-industrialization. [Keywords:] cefepime; GCLE; one-pot method; synthesis ABSTRACT Cefepime was synthesized from GCLE via nucleophilic substitution on C-3 position, one-pot cleavage of C-7 and C-2 protecting group and condensation on C-7 position. A good quality product was obtained with the total yield 36%. This method was simple, rapid and easy to scale up industrially. KEY WORDS Cefepime; GCLE; One-pot reaction; Synthesis Cephalosporin antibiotics from first-generation product development to the fourth generation, or even the fifth-generation research and development trend. Has been listed fourth-generation cephalosporins against Gram-negative bacteria, especially Enterobacteriaceae, Pseudomonas aeruginosa has good activity, while maintaining the right of the role of Gram-positive bacteria, can not be compared with the previous three generations of anti-bacterial characteristics of . Cefepime for the fourth-generation cephalosporins, was first proposed by Bristol-Myers Squibb Company developed in 1993, first in the Swedish market, its unique structure, with high efficiency, broad-spectrum, low toxicity, anti-bacterial characteristics of β -lactam enzymes , and has good pharmacokinetic properties in clinical practice is mainly used for respiratory tract infections, urinary tract infections, skin and soft tissue infections, surgical infections, meningitis, appendicitis, and the treatment of sepsis and other bacterial infections. In September 1983 for the first time published a synthesis of cefepime [1], methods to 7 - phenyl-acetyl amino cephalosporins prepared from the starting