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Synlett 1997; 1997(8): 959-961
DOI: 10.1055/s-1997-936
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Functionalised Pyrazoles through a Facile One-Pot Procedure from N-Tosyl-N-propargyl-hydrazine and Aryl Iodides or Vinyl Triflates

Sandro Cacchi* , Giancarlo Fabrizi, Antonella Carangio
  • *Dipartimento di Studi di Chimica e Tecnologia delle Sostanze Biologicamente Attive, Università “La Sapienza”, P.le A. Moro 5, 00185 Roma, Italy, Fax: +39 (6) 4991.2780; e-mail: cacchi@axrma.uniroma1.it
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Publikationsdatum:
31. Dezember 2000 (online)

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Functionalised pyrazoles have been prepared in good overall yield through a facile one-pot procedure. The synthesis includes the palladium-catalysed coupling of the readily available N-tosyl-N-propargylhydrazine with aryl iodides or vinyl triflates, the palladium-catalysed annulation of the resulting N-tosyl-N-(1-aryl/vinyl-1-propyn-3-yl)hydrazine and exposure of the reaction mixture arising from the annulation step to KOBut.

pyrazoles - palladium catalysis - coupling - annulation - aryl iodides - vinyl triflates

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