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Two-step synthesis of structure-diverse d-galactose conjugates and polymeric prodrugs of floxuridine via controllable regioselective enzymatic acylation of 3′- or 5′-OH group of floxuridine

Paper ID Volume ID Publish Year Pages File Format Full-Text
17881 42703 2008 7 PDF Available
Title
Two-step synthesis of structure-diverse d-galactose conjugates and polymeric prodrugs of floxuridine via controllable regioselective enzymatic acylation of 3′- or 5′-OH group of floxuridine
Abstract

We achieved an effective way of controllable regioselective acylation of primary or secondary hydroxyl group of floxuridine with different enzymes. Polymerizable 5′-O-acyl-floxuridine derivatives were synthesized by CAL-B (immobilized lipase from Candida antarctica) in acetonitrile or subtilisin in pyridine, and the 3′-O-acyl-floxuridine derivatives by PSL-C (Pseudomonas cepacia, immobilized) in THF with high selectivity and yields. These resulting monomers were subjected to the further transformations in the second step, i.e. chemo-polymerization in DMF initiated by azobisisobutyronitrile to give polymeric prodrugs with the same backbone and different branch position, and enzymatic conjugation of d-galactose for the synthesis of d-galactose–floxuridine conjugates with acylation position-diversity, which were potential targeting drugs.

Keywords
Controllable regioselectivity; d-Galactose–floxuridine conjugates; Floxuridine; Polymeric prodrugs; Enzymatic synthesis
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Two-step synthesis of structure-diverse d-galactose conjugates and polymeric prodrugs of floxuridine via controllable regioselective enzymatic acylation of 3′- or 5′-OH group of floxuridine
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Publisher
Database: Elsevier - ScienceDirect
Journal: Enzyme and Microbial Technology - Volume 42, Issue 5, 4 April 2008, Pages 414–420
Authors
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Subjects
Physical Sciences and Engineering Chemical Engineering Bioengineering
Get Full-Text Now
Don't Miss Today's Special Offer
Price was $35.95
You save - $31
Price after discount Only $4.95
100% Money Back Guarantee
Full-text PDF Download
Online Support
Any Questions? feel free to contact us