Selective hydrolysis of 2,4-diaminopyrimidine systems: a theoretical and experimental insight into an old rule

J Org Chem. 2001 Jan 12;66(1):192-9. doi: 10.1021/jo0056390.

Abstract

Hydrolysis of the amino groups in condensed 2,4-diaminopyrimidine systems (1) has been used as a common method for the synthesis of oxo-substituted pyrimidines. In particular, the treatment with 6 M HCl usually yields exclusively the 2-amino-4-oxopyrimidine isomer (2). During our work, we found that the hydrolysis of the amino groups present in some condensed 2,4-diaminopyrimidine systems unexpectedly afforded exclusively the 4-amino-2-oxopyrimidine isomer (3). In this paper, we present the experimental work and ab initio calculations carried out to understand this discrepancy. As a part of such study, eight compounds containing a 2,4-diaminopyrimidine moiety were calculated in gas phase and in aqueous solution, and some acid hydrolyses were reexamined. Results showed that the presence of an electron-donating nitrogen linked to C6 of the 2,4-diaminopyrimidine ring changes the preferred hydrolysis site to yield the 4-amino-2-oxopyrimidine isomer.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemical Phenomena
  • Chemistry, Physical
  • Folic Acid Antagonists / chemical synthesis
  • Folic Acid Antagonists / chemistry*
  • Hydrolysis
  • Indicators and Reagents
  • Pyrimidines / chemical synthesis
  • Pyrimidines / chemistry*
  • Tetrahydrofolate Dehydrogenase*

Substances

  • Folic Acid Antagonists
  • Indicators and Reagents
  • Pyrimidines
  • 2,4-diaminopyrimidine
  • Tetrahydrofolate Dehydrogenase