Ketonitriles as Intermediates for the Synthesis of Antiparasitic Drugs
Glover, Johnny III
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Objective: Synthesize b-ketonitriles as intermediates towards an effective drug to counteract the parasitic tropical disease leishmaniasis. Introduction: Diaminopyrimidines have been used as drugs against parasitic diseases like malaria, and less notably against leishmaniasis. Increased resistance, decreased efficacy, and severe side effects have been observed in the current treatment regimen highlighting the need for new drugs against those diseases. Methods: Six esters reacted with four different nitriles in the presence of potassium tert-butoxide using tetrahydrofuran as solvent to form b-ketonitriles. Results: Twenty-four b-ketonitriles were synthesized using a microwave reactor, with yields varying from 30 to 72%. Conclusion: Microwave conditions are appropriate for the synthesis of b-ketonitriles. Yields were variable, with starting materials containing amino groups resulting in lower yields of solid compounds of difficult purification.