1337482-15-1Relevant articles and documents
The protecting-group free selective 3′-functionalization of nucleosides
McCabe Dunn, Jamie M.,Reibarkh, Mikhail,Sherer, Edward C.,Orr, Robert K.,Ruck, Rebecca T.,Simmons, Bryon,Bellomo, Ana
, p. 2804 - 2810 (2017)
The direct and chemoselective 3′-phosphoramidation, phosphorylation and acylation of nucleosides are described. Upon the discovery of a novel 3′-phosphorylamidation of therapeutic nucleoside analogues with DBU, we explored the mechanism of this rare selectivity through a combination of NMR spectroscopy and computational studies. The NMR and computational findings allowed us to develop a predictive computational model that accurately assesses the potential for 3′-functionalization for a broad range of nucleosides and nucleoside mimetics. The synthetic utility of this model was exemplified by demonstration on a broad scope of nucleosides and electrophiles yielding targets that were previously only accessible via a protection/deprotection sequence or an enzymatic approach.
PROCESS FOR MAKING PHOSPHORUS-CONTAINING NUCLEOSIDE PRODRUG COMPOUNDS
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Page/Page column 39; 41, (2017/02/24)
The present invention is directed to processes for making Compounds of Formula (IV): (IV) and salts thereof, wherein B, X, R1, R2, R3 and R4 are defined herein.