A practical synthesis of nitrocefin
A practical synthesis of nitrocefin
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DOI：
10.1021/jo0487395
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发表时间：
2005-01-07
影响因子：
3.6
通讯作者：
Mobashery, S
中科院分区：
文献类型：
--
作者：
Lee, M;Hesek, D;Mobashery, S
硝头孢菌素是青霉素结合蛋白（PBP）和β-内酰胺酶活性高通量和低通量测定的关键试剂，前者用于发现抗生素，后者用于β-内酰胺抗生素耐药决定因素的抑制剂。该化合物可商购获得，但由于其合成路线迂回而过于昂贵。本文描述了头孢硝肟的三步合成，总收率为44%。这是一条合成药物发现关键试剂的实用路线。
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 discover.