立体中心
催化作用
化学
不对称氢化
组合化学
对映选择合成
衍生工具(金融)
全合成
立体化学
有机化学
业务
财务
作者
Yang Zhi,Yu Chen,Lin-Xi Wan,Xiangling Cen,Pei Tang,Fen‐Er Chen
摘要
A catalytic asymmetric total synthesis of avibactam and relebactam, two marketed diazabicyclooctane (DBO) β-lactamase inhibitors (BLIs), has been accomplished. An important feature of this study is the creation of a stereogenic center by using Rh-catalysed asymmetric hydrogenation, affording the crucial α-amino acid ester derivative with high-level enantiocontrol (99% ee). Furthermore, the adoption of flow technologies for the assembly of a majority of intermediates significantly achieves a faster preparation and greater synthetic efficiency than corresponding batch procedures.
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