Synthesis of oligonucleotides containing thiazole and thiazole N-oxide nucleobases

Org Lett. 2002 Mar 21;4(6):877-80. doi: 10.1021/ol017003g.

Abstract

[reaction: see text] The thiazole C-nucleoside analogue was synthesized by the Hantzsch cyclization method to form the thiazole ring and was then converted to the thiazole N-oxide C-nucleoside analogue by peracid oxidation of the heterocycle nitrogen. Incorporation of the thiazole and thiazole N-oxide phosphoramidites into DNA was successful though significant deoxygenation of the N-oxide occurred during DNA assembly. The mechanism proposed for the reduction of the thiazole N-oxide to thiazole involves the formation of an N-oxide phosphite ester.

Publication types

  • Research Support, Non-U.S. Gov't
  • Research Support, U.S. Gov't, P.H.S.

MeSH terms

  • Crystallography, X-Ray
  • Models, Molecular
  • Nucleosides / chemistry*
  • Oligonucleotides / chemical synthesis*
  • Oligonucleotides / chemistry
  • Thiazoles / chemistry*

Substances

  • Nucleosides
  • Oligonucleotides
  • Thiazoles