New methods for the synthesis of spirocyclic cephalosporin analogues
收藏Scottish Government Open Data Portal2021-10-01 更新2026-05-09 收录
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https://www.research.ed.ac.uk/en/datasets/new-methods-for-the-synthesis-of-spirocyclic-cephalosporin-analog
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资源简介：
Spiro compounds provide attractive targets in drug discovery due to their inherent three-dimensional structures, which enhance protein interactions, aid solubility and facilitate molecular modelling. However, synthetic methodology for the spiro-functionalisation of important classes of penicillin and cephalosporin β-lactam antibiotics is comparatively limited. We report a novel method for the generation of spiro-cephalosporin compounds through a Michael-type addition to the dihydrothiazine ring. Coupling of a range of catechols is achieved under mildly basic conditions (K2CO3, DMF), giving the stereoselective formation of spiro-cephalosporins (d.r. 14:1 to 8:1) in moderate to good yields (28-65%).
创建时间：
2021-10-01
