Palladium-mediated C–N, C–C, and C–O functionalization of azolopyrimidines: a new total synthesis of variolin B

نویسندگان

  • Alejandro Baeza
  • Javier Mendiola
  • Carolina Burgos
  • Julio Alvarez-Builla
  • Juan J. Vaquero
چکیده

A new total synthesis of the alkaloid variolin B is achieved by a selective and sequential palladium-mediated functionalization of a trihalo-substituted pyrido[30,20:4,5]pyrrolo[1,2-c]pyrimidine. This intermediate is obtained by a new heterocyclization reaction between an appropriate bromomethyl azaindole and N-tosylmethyl dichloroformimide. The methodology may be effective for the synthesis of some analogs by substitution on the relatively unexplored C4 and C9 positions of the alkaloid. 2008 Elsevier Ltd. All rights reserved.

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تاریخ انتشار 2008