4.7 Article

Hypervalent Iodine/HF Reagents for the Synthesis of 3-Fluoropyrrolidines

期刊

JOURNAL OF ORGANIC CHEMISTRY
卷 82, 期 22, 页码 11721-11726

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AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.7b01266

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  1. JSPS KAKENHI [16K05703]
  2. Grants-in-Aid for Scientific Research [16K05703] Funding Source: KAKEN

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The intramolecular aminofluorination of homoallylamine derivatives using a reagent system of PhI(OAc)(2) and Py.HF in CH2Cl2 at room temperature for 5 h gave N-tosyl-3-fluoropyrrolidines in good to high yields. Furthermore, the catalytic aminofluorination was furnished by the reaction using p-iodotoluene as a catalyst in the presence of Py.HF as a fluorine source and mCPBA as a terminal oxidant

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