Efficient construction of pyrazolo[1,5-a]pyrimidine scaffold and its exploration as a new heterocyclic fluorescent platform

J Fluoresc. 2008 Mar;18(2):357-63. doi: 10.1007/s10895-007-0275-0. Epub 2007 Nov 16.

Abstract

An efficient, fast and facile pyrazolo[1,5-a]pyrimidine synthetic protocol has been established by the condensation of aminopyrazoles with 1,3-dicarbonyl components in AcOH/H(2)SO(4) system. The pyrazolo[1,5-a]pyrimidine sulfides were selectively oxidized to the sulfones via a temperature-controlled stepwise oxidative fashion. The correlation between the substitution patterns of these pyrazolo[1,5-a]pyrimidines and their fluorescent spectroscopic properties were further examined, which provided the fundamentals for their potential applications in the development of new fluorescent probes. Red-shifts were easily achieved by the incorporation of unsaturated groups at the 5- and 7-positions, which suggested an approach for synthesizing long wavelength pyrazolo[1,5-a]pyrimidine dyes. The fluorescent spectroscopic properties were found to be sensitive to the hydroxy-containing and carbonyl-containing media such as alcohol and acetone, which helps to confirm the promising perspectives of further investigations in this area.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Binding, Competitive
  • Fluorescent Dyes / chemical synthesis*
  • Fluorescent Dyes / chemistry*
  • Molecular Structure
  • Pyrazoles / chemistry*
  • Pyrimidines / chemical synthesis*
  • Pyrimidines / chemistry
  • Spectrometry, Fluorescence
  • Structure-Activity Relationship

Substances

  • Fluorescent Dyes
  • Pyrazoles
  • Pyrimidines