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Org Lett. 2014 Aug 15;16(16):4186-9. doi: 10.1021/ol5018855. Epub 2014 Jul 25.

Synthesis of multisubstituted 2-aminopyrroles/pyridines via chemoselective Michael addition/intramolecular cyclization reaction.

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  • 1State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences , 555 Zuchongzhi Road, Shanghai, 201203, China.


A facile and efficient synthetic strategy to construct polysubstituted 2-aminopyrroles/pyridines was developed via chemoselective Michael addition/intramolecular cyclization reaction under very mild conditions. It suggested that the chemoselectivity of the process could be controlled by the leaving ability of the halides.

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