Skip to main content
U.S. Department of Energy
Office of Scientific and Technical Information

Synthesis and separation of diastereomers of ribonucleoside 5{prime}-({alpha}-P-borano)triphosphates

Journal Article · · Journal of Organic Chemistry
DOI:https://doi.org/10.1021/jo972002g· OSTI ID:659067
; ; ;  [1]
  1. Duke Univ., Durham, NC (United States)
Nucleoside boranophosphates, in which one of the phosphate oxygens is replaced by a borane group, are isoionic and isoelectronic analogues of naturally occurring nucleotides. Boranophosphates also are biochemically important congeners of phosphorothioates and methylphosphonates. The authors have developed a convenient one-pot method to synthesize the set of ribonucleoside (A, U, G, and C) 5{prime}-({alpha}-P-borano)triphosphates. Phosphitylation of the 2{prime},3{prime}-protected ribonucleoside with 2-chloro-4H-1,3,2-benzodioxaphosphorin-4-one gives the 5{prime}-phosphite intermediate 2 which undergoes in situ substitution in the presence of pyrophosphate to give the cyclic intermediate, P{sup 2},P{sup 3}-dioxo-P{sup 1}-ribonucleosidylcyclotriphosphate 3. Immediate oxidation of compound 3 with amine{center_dot}borane complex results in ribonucleoside 5{prime}-({alpha}-P-borano)cyclotriphosphate 4. Subsequent reaction of compound 4 with water followed by ammonium hydroxide yields the crude product as a diastereomeric mixture of ribonucleoside 5{prime}-({alpha}-P-borano)triphosphate 6. Pure compound 6 is isolated in 30--45% overall yield using ion-exchange chromatography. The separation of two diastereomers of ribonucleoside 5{prime}-({alpha}-P-borano)triphosphate 6 is achieved by reverse phase HPLC.
Sponsoring Organization:
USDOE, Washington, DC (United States)
DOE Contract Number:
FG05-94ER61882; FG02-97ER62376
OSTI ID:
659067
Journal Information:
Journal of Organic Chemistry, Journal Name: Journal of Organic Chemistry Journal Issue: 17 Vol. 63; ISSN JOCEAH; ISSN 0022-3263
Country of Publication:
United States
Language:
English