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- W2080998033 abstract "Efficient protocols for the selective synthesis of monosaccharide derivatives and polymeric prodrugs of 5-fluorouridine (5-FUR) have been developed. Firstly, transesterification of 5-FUR and divinyl dicarboxylates ranging from 4 to 10 carbon atoms were performed under the catalysis of Candida antarctica lipase acrylic resin in anhydrous THF at 50 °C, respectively. A series of vinyl 5-FUR esters were prepared, with high acylation regioselectivity at 5′-OH. The influences of reaction parameters including enzyme, solvents, molar ratio of substrates, reaction time, the carbon length of acyl donor and reaction temperature were investigated in details. And then, protease-catalyzed highly regioselective acylation of d-glucose, d-mannose and d-galactose with vinyl esters of 5-FUR gave 5-FUR-saccharide derivatives successfully. Moreover, a series of polymeric prodrugs of 5-FUR with the different linker lengths were prepared by the chemo-polymerization of vinyl 5-FUR esters in DMF initiated by azobisisobutyronitrile (AIBN)." @default.
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- W2080998033 date "2008-08-01" @default.
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- W2080998033 title "Synthesis of monosaccharide derivatives and polymeric prodrugs of 5-fluorouridine via two-step enzymatic or chemo-enzymatic highly regioselective strategy" @default.
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- W2080998033 doi "https://doi.org/10.1016/j.molcatb.2007.12.023" @default.
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