Skip to main content
Article thumbnail
Location of Repository

Studies in the synthesis of pyrimidines, pyrazoles, and pyrazolo pyrimidines. New syntheses of 1, 3 and 5 substituted pyrazolo [3, 4-d] pyrimidines, including glycosides related to naturally occurring pyrimidines, imidazoles, purines and their nucleoside derivatives.

By Brian G. Hildick


Some compounds, analogous to those found in naturally\ud occurring systems, are found to possess chemotherapeutic activity.\ud Some, in the form of their nucleoside or nucleotide derivatives,\ud are valuable antimetabolites in that they may block normal RNA\ud or DNA polymerisation, or may be incorporated into nucleic acids\ud to form fraudulent, but not necessarily defective, polymers.\ud Modification of natural ring systems, with a view to promoting\ud chemotherapeutic activity is therefore of considerable interest;\ud variation in the position and nature of the modification or ring\ud substituent having a marked effect on chemotherapeutic activity.\ud It is the purpose of this thesis to suggest methods for the\ud facile synthesis of various uracils, pyrazoles and pyrazolo\ud [3,4-d]\ud -\ud pyrimidines with alkyl, aryl and glycosyl substituents such that\ud the nature of the ring substituents is easily varied.\ud To this end a number of ethoxymethylene reagents were prepared\ud which, by reaction with primary amines and hydrazines, would give\ud acyclic intermediates capable of easy cyclisation into the uracil,\ud pyrazole and pyrazolo\ud [3,4-d]\ud pyrimidine ring systems. Variation in\ud the nature of specific substituents being determined by the choice\ud of amine or hydrazine, other substituents being varied by modification\ud of the original reagent.S.R.G

Topics: Pyrimidines, Imidazoles, Purines, Chemical synthesis, Pyrazoles, Pyrazolo pyrimidines, Chemotherapeutic activity
Publisher: Board of Physical Sciences
Year: 1978
OAI identifier:
Provided by: Bradford Scholars
Download PDF:
Sorry, we are unable to provide the full text but you may find it at the following location(s):
  • (external link)
  • (external link)
  • Suggested articles

    To submit an update or takedown request for this paper, please submit an Update/Correction/Removal Request.