基于碱的 2H-氮丙啶的级联取代-环化反应：高取代恶唑的合成。
Base-Mediated Cascade Substitution-Cyclization of 2H-Azirines: Access to Highly Substituted Oxazoles.
机构信息
School of Chemical Engineering & Pharmaceutics, Henan University of Science and Technology , Luoyang 471003, Henan, China.
State Key Laboratory and Institute of Elemento-Organic Chemistry, Nankai University , Tianjin 300071, China.
出版信息
Org Lett. 2017 Jul 7;19(13):3370-3373. doi: 10.1021/acs.orglett.7b01305. Epub 2017 Jun 13.
A novel strategy to synthesize highly functionalized oxazoles has been successfully developed via a base-mediated intermolecular substitution between 2-acyloxy-2H-azirines and N-nucleophile or O-nucleophile with a subsequent ring expansion of a 2H-azirine intermediate. This method provides straightforward access to highly substituted oxazoles with high efficiency and excellent functional group compatibility under metal-free reaction conditions.
一种新的策略，通过 2-酰氧基-2H-氮丙啶与 N-亲核试剂或 O-亲核试剂之间的碱介导的分子间取代反应，并随后进行 2H-氮丙啶中间体的环扩张，成功地合成了高度官能化的恶唑。该方法在无金属反应条件下，提供了高效、高官能团兼容性的高度取代恶唑的直接途径。
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