Parallel synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones on solid-phase Article

Hu, M, Huang, W, Giulianotti, MA et al. (2013). Parallel synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones on solid-phase . 15(7), 335-339. 10.1021/co400064d

cited authors

  • Hu, M; Huang, W; Giulianotti, MA; Houghten, RA; Yu, Y

abstract

  • A parallel solid-phase synthesis of 1,6-disubstituted-1,2,4-triazin-3-ones from MBHA resin is described. The reduction of resin-bound nitrosamino acids provides hydrazines efficiently without affecting the amide bond. The trityl protected hydrazine is then reduced with borane, and cyclized with 1,1-carbonyldiimidazole. The desired products are cleaved from their solid support and obtained in good yield and purity. This methodology is of value for the rapid parallel preparation of these potentially bioactive molecules. © 2013 American Chemical Society.

publication date

  • July 8, 2013

Digital Object Identifier (DOI)

start page

  • 335

end page

  • 339

volume

  • 15

issue

  • 7