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Azetidine and cyclopropylamine in the “1,2,4-triazine” methodology for the synthesis of α-functionalized 2,2′-bipyridines

  • Ya. K. Shtaitz,
  • M. I. Valieva,
  • E. D. Ladin,
  • A. Rammohan,
  • K. D. Krasnoperova,
  • N. A. Belyaev,
  • D. S. Kopchuk,
  • G. V. Zyryanov,
  • V. L. Rusinov

摘要

Functionalization of 3-(2-pyridyl)-1,2,4-triazines with small (aza)cyclic compounds (azetidine and cyclopropylamine) via nucleophilic ipso-substitution of the cyano group and subsequent transformation of the 1,2,4-triazine ring into pyridine one via the aza-Diels—Alder reaction were explored. The successful proceeding of such a transformation depended on the structure of the nucleophilic residue: both steps were successfully implemented upon using a cyclopropylamine derivative, while in the case of azetidine-containing 1,2,4-triazines, there was only the resinification of the reaction mass.