A Concise Route to MK-4482 (EIDD-2801) from Cytidine: Part 2
David R. Snead, Vijayagopal Gopalsamuthiram, Corshai Williams, Jeffrey S. Noble, Timothy F. Jamison, B. Frank Gupton
Abstract
Abstract A new route to MK-4482 was developed. The route replaces uridine with the more available and less expensive cytidine. Low-cost, simple reagents are used for the chemical transformations, and the yield is improved from 17% to 44%. A step is removed from the longest linear sequence, and these advancements are expected to expand access to MK-4482 should it become a viable drug substance.
Topics & Concepts
CytidineChemistryReagentYield (engineering)Combinatorial chemistryBiochemistryOrganic chemistryPhysicsThermodynamicsEnzymeChemical Synthesis and AnalysisChemical Reactions and IsotopesCancer therapeutics and mechanisms