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An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals

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dc.contributor.author Gordon, GER
dc.contributor.author Bode, ML
dc.contributor.author Visser, Daniel F
dc.contributor.author Lepuru, MJ
dc.contributor.author Zeevaart, JG
dc.contributor.author Ragubeer, N
dc.contributor.author Ratsaka, M
dc.contributor.author Walwyn, DR
dc.contributor.author Brady, D
dc.date.accessioned 2012-04-18T09:24:03Z
dc.date.available 2012-04-18T09:24:03Z
dc.date.issued 2011-01
dc.identifier.citation Gordon, GER, Bode, ML, Visser, DF, Lepuru, MJ, Zeevaart, JG, Ragubeer, N, Ratsaka, M, Walwyn, DR and Brady, D. 2011. An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals. Organic Process Research & Development, vol. 15(1), pp 258-265 en_US
dc.identifier.issn 1083-6160
dc.identifier.uri http://pubs.acs.org/doi/abs/10.1021/op100208x
dc.identifier.uri http://pubs.acs.org/doi/pdf/10.1021/op100208x
dc.identifier.uri http://hdl.handle.net/10204/5784
dc.description Copyright: 2011 American Chemical Society. This is an ABSTRACT ONLY. en_US
dc.description.abstract A chemo-enzymatic method for production of ß-thymidine, an intermediate in the synthesis of antiretrovirals, is described. Guanosine and thymine were converted by means of enzymatic transglycosylation to yield 5-methyluridine (5-MU), which was reproducibly synthesised at a 10-20-L scale in 85% yield at a final product concentration of 80 g·L-1. A downstream processing (DSP) protocol was designed to remove reaction components interfering with the subsequent synthetic step. The crystallised 5-MU produced in the biocatalytic reaction was found to behave similarly to commercially available 5-MU, and the integration of the initial biocatalytic and subsequent three-step chemical process to ß-thymidine was successfully demonstrated at bench scale. en_US
dc.language.iso en en_US
dc.publisher American Chemical Society en_US
dc.relation.ispartofseries Workflow;5752
dc.subject ß-Thymidine en_US
dc.subject Biocatalysis en_US
dc.subject Antiretrovirals en_US
dc.subject Chemo-enzymatic en_US
dc.title An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals en_US
dc.type Article en_US


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