6533b7d6fe1ef96bd1266769
RESEARCH PRODUCT
A concise route to MK-4482 (EIDD-2801) from cytidine.
Till OpatzFlavio S. P. CardosoFrank GuptonJule-phillip DietzDinesh J. PaymodeGrace P. AhlqvistTobias LucasTimothy F. JamisonDavid R. SneadN. VasudevanCatherine P. Mcgeoughsubject
010405 organic chemistryAcylationMetals and AlloysCytidineGeneral ChemistryCytidine010402 general chemistryHydroxylamines01 natural sciencesCombinatorial chemistryCatalysisUridine0104 chemical sciencesSurfaces Coatings and FilmsElectronic Optical and Magnetic MaterialsAcylationchemistry.chemical_compoundKineticschemistryYield (chemistry)Materials ChemistryCeramics and CompositesStep countAminationdescription
A two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an esterification and hydroxamination of cytidine. The selective acylation and direct amination eliminate the need for protecting and activating groups and proceed in overall yield of 75%, a significant advancement over the reported yield of 17%. The step count is reduced from five transformations to two, and expensive uridine is replaced with the more available cytidine.
| year | journal | country | edition | language |
|---|---|---|---|---|
| 2020-10-09 | Chemical communications (Cambridge, England) |