Synthesis of 8-Substituted Purines as Antimalarials.
Final technical rept. 1 Jan 73-31 Mar 74,
EXXON RESEARCH AND ENGINEERING CO LINDEN N J GOVERNMENT RESEARCH LAB
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The synthesis, properties and biological test data of potential antimalarial drugs based on 8-substituted purines is described. During the period of performance 33 purines and 8 intermediates were prepared. These were of 3 different types 1 2,6-diaminopurines with various 8-substituents 2 9-substituted purines and 3 miscellaneous purines mostly containing halogen atoms. A variety of synthesis methods are described. These include ring closure of acylamino pyrimidines, nucleophilic displacement of groups on pre-formed purines and oxidation of thiol groups to sulfoxides and sulfones. Correlations between chemical structure and reactivity are noted where appropriate. Physical properties and their effects on purification procedures are described. Biological test data for about 12 of the compounds submitted are summarized. None of the test compounds were active. Modified author abstract
- Organic Chemistry