A Practical Synthesis of Nitrocefin

摘要

Nitrocefin is a key reagent for high and low throughput assays of the activities of penicillin-binding proteins(PBPs)and beta-lactamases,the former used for discovery of antibiotics and the latter for inhibitors of resistance determinants for beta-lactam antibiotics.This compound is commercially available but is prohibitively expensive because of the circuitous routes to its synthesis.We describe herein a three-step synthesis of nitrocefin that gives an overall yield of"44%.This is a practical route to the synthesis of this key reagent for drug discovery.