期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 56, 期 35, 页码 10573-10576出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201705746
关键词
chiral phosphoric acids; cycloaddition; heterocycles; hydrogen bonds; intramolecular Povarov reaction
资金
- CNRS
- Saclay University
A highly efficient catalytic enantioselective intramolecular Povarov reaction was developed with primary anilines as 2-azadiene precursors. A wide variety of angularly fused azacycles were obtained without column chromatography in high to excellent yields and with excellent diastereo- and enantioselectivity (d.r. > 99:1 and up to e.r. 99:1). Furthermore, the catalyst loading could be lowered to 1 mol %, and the obtained azacycles could be used as key intermediates for further transformationstrans to generate additional molecular diversity.
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