Liu Jian-Bo, Xu Xiu-Hua, Qing Feng-Ling
Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Science , 345 Lingling Lu, Shanghai 200032, China.
College of Chemistry, Chemical Engineering and Biotechnology, Donghua University , 2999 North Renmin Lu, Shanghai 201620, China.
Org Lett. 2015 Oct 16;17(20):5048-51. doi: 10.1021/acs.orglett.5b02522. Epub 2015 Sep 29.
The development of an efficient and practical method for the preparation of alkyl trifluoromethyl ethers is urgently demanding. The silver-mediated oxidative O-trifluoromethylation of primary, secondary, and tertiary alcohols with TMSCF3 under mild reaction conditions is established to provide a novel approach to a broad range of alkyl trifluoromethyl ethers. Further, this method is applied to the late-stage O-trifluoromethylation of complex natural products and prescribed pharmaceutical agents.
迫切需要开发一种高效实用的制备烷基三氟甲基醚的方法。已建立了在温和反应条件下,银介导的伯醇、仲醇和叔醇与三甲基硅基三氟甲烷(TMSCF3)的氧化O-三氟甲基化反应,为制备多种烷基三氟甲基醚提供了一种新方法。此外,该方法还应用于复杂天然产物和处方药的后期O-三氟甲基化反应。