通过铑催化的 C(sp )-H 功能化/环化反应的不对称合成螺吡唑酮。
Asymmetric Synthesis of Spiropyrazolones by Rhodium-Catalyzed C(sp )-H Functionalization/Annulation Reactions.
机构信息
State Key Laboratory of Organometallic Chemistry, Shanghai Institute of Organic Chemistry, University of Chinese Academy of Sciences, Chinese Academy of Sciences, 345 Lingling Lu, Shanghai, 200032, China.
Collaborative Innovation Center of Chemical Science and Engineering (Tianjin), Tianjin, 300072, China.
出版信息
Angew Chem Int Ed Engl. 2017 Apr 10;56(16):4540-4544. doi: 10.1002/anie.201700021. Epub 2017 Mar 22.
Rhodium-catalyzed C(sp )-H functionalization reactions of 4-aryl-5-pyrazolones followed by [3+2] annulation reactions with alkynes provide rapid access to highly enantioenriched five-membered-ring 4-spiro-5-pyrazolones. The use of a chiral SCpRh catalyst enabled the synthesis of a large range of spiropyrazolones with all-carbon quaternary stereogenic centers in up to 99 % yield and 98 % ee from readily available substrates.
铑催化的 4-芳基-5-吡唑酮的 C(sp 3 )-H 官能化反应，接着与炔烃进行[3+2]环加成反应，可快速得到高对映选择性的五元环 4-螺-5-吡唑酮。使用手性 SCpRh 催化剂，可从易得的底物中以高达 99%的产率和 98%的对映选择性合成具有全碳季碳手性中心的各种螺吡唑酮。
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