Gordon, GERBode, MLVisser, Daniel FLepuru, MJZeevaart, JGRagubeer, NRatsaka, MWalwyn, DRBrady, D2012-04-182012-04-182011-01Gordon, 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 258-2651083-6160http://pubs.acs.org/doi/abs/10.1021/op100208xhttp://pubs.acs.org/doi/pdf/10.1021/op100208xhttp://hdl.handle.net/10204/5784Copyright: 2011 American Chemical Society. This is an ABSTRACT ONLY.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.enß-ThymidineBiocatalysisAntiretroviralsChemo-enzymaticArticleGordon, 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/10204/5784Gordon, 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/10204/5784Gordon 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.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 -