Li Zheyao, Zhang Huiwen, Zhao Lin, Ma Yueyue, Wu Qiufang, Ren Haosong, Lin Zhongren, Zheng Jun, Yu Xinhong
Engineering Research Centre of Pharmaceutical Process Chemistry, Ministry of Education, Shanghai Key Laboratory of New Drug Design, School of Pharmacy and State Key Laboratory of Bioengineering Reactors, East China University of Science and Technology, 130 Meilong Road, Shanghai 200237, China.
School of Biomedical and Pharmaceutical Sciences, Guangdong University of Technology, 100 West Waihuan Road, Guangzhou 510006, Guangdong, China.
Chem Commun (Camb). 2024 Mar 26;60(26):3579-3582. doi: 10.1039/d4cc00116h.
A DMP-initiated metal-free effective β,γ-asymmetric spirocyclopropanation of propanols strategy using oxidative iminium activation is described. This process has been realized by a synergistic amine-catalyzed one-pot cascade oxidation-Michael addition cyclopropanation for "one-pot" access to various spirocyclopropyl propionaldehydes/propanols from diverse 3-arylpropanols and α-brominated active methylene compounds under mild conditions and with high enantioselectivity (ee up to >99%).
描述了一种由DMP引发的、使用氧化亚胺活化的无金属有效β,γ-不对称环丙烷化丙醇的策略。该过程通过协同胺催化的一锅串联氧化-迈克尔加成环丙烷化反应得以实现，能够在温和条件下、以高对映选择性（对映体过量高达>99%）“一锅法”从各种3-芳基丙醇和α-溴代活性亚甲基化合物制备各种螺环丙基丙醛/丙醇。
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