dc.contributor.author |
Gordon, GER
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dc.contributor.author |
Bode, ML
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dc.contributor.author |
Visser, Daniel F
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dc.contributor.author |
Lepuru, MJ
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dc.contributor.author |
Zeevaart, JG
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dc.contributor.author |
Ragubeer, N
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dc.contributor.author |
Ratsaka, M
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dc.contributor.author |
Walwyn, DR
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dc.contributor.author |
Brady, D
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dc.date.accessioned |
2012-04-18T09:24:03Z |
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dc.date.available |
2012-04-18T09:24:03Z |
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dc.date.issued |
2011-01 |
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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
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|
dc.identifier.uri |
http://pubs.acs.org/doi/pdf/10.1021/op100208x
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dc.identifier.uri |
http://hdl.handle.net/10204/5784
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|
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 |
dc.identifier.apacitation |
Gordon, G., Bode, M., Visser, D. F., Lepuru, M., Zeevaart, J., Ragubeer, N., ... Brady, D. (2011). An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals. http://hdl.handle.net/10204/5784 |
en_ZA |
dc.identifier.chicagocitation |
Gordon, GER, ML Bode, Daniel F Visser, MJ Lepuru, JG Zeevaart, N Ragubeer, M Ratsaka, DR Walwyn, and D Brady "An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals." (2011) http://hdl.handle.net/10204/5784 |
en_ZA |
dc.identifier.vancouvercitation |
Gordon G, Bode M, Visser DF, Lepuru M, Zeevaart J, Ragubeer N, et al. An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals. 2011; http://hdl.handle.net/10204/5784. |
en_ZA |
dc.identifier.ris |
TY - Article
AU - Gordon, GER
AU - Bode, ML
AU - Visser, Daniel F
AU - Lepuru, MJ
AU - Zeevaart, JG
AU - Ragubeer, N
AU - Ratsaka, M
AU - Walwyn, DR
AU - Brady, D
AB - 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.
DA - 2011-01
DB - ResearchSpace
DP - CSIR
KW - ß-Thymidine
KW - Biocatalysis
KW - Antiretrovirals
KW - Chemo-enzymatic
LK - https://researchspace.csir.co.za
PY - 2011
SM - 1083-6160
T1 - An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals
TI - An integrated chemo-enzymatic route for preparation of ß-thymidine, a key intermediate in the preparation of antiretrovirals
UR - http://hdl.handle.net/10204/5784
ER -
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en_ZA |