Para-Selective Gold-Catalyzed Direct Alkynylation of Anilines

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Para-selective gold-catalyzed direct alkynylation of anilines.

A method for the para-selective alkynylation of anilines is reported using AuCl as catalyst and triisopropylsilylethynyl-1,2-benziodoxol-3(1H)-one (TIPS-EBX) as an electrophilic acetylene equivalent. Para-alkynyl anilines substituted at positions 2 or 3 were obtained in one step from simple anilines under mild conditions (room temperature to 60 °C) under air. The methodology could also be exten...

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ژورنال

عنوان ژورنال: Organic Letters

سال: 2012

ISSN: 1523-7060,1523-7052

DOI: 10.1021/ol203289v