An Integrated Chemo-enzymatic Route for Preparation of β-Thymidine, a Key Intermediate in the Preparation of Antiretrovirals

…, JG Zeevaart, N Ragubeer, M Ratsaka…

Index: Gordon, Gregory E. R.; Bode, Moira L.; Visser, Daniel F.; Lepuru, M. Jerry; Zeevaart, Jacob G.; Ragubeer, Nasheen; Ratsaka, Molala; Brady, Dean; Walwyn, David R. Organic Process Research and Development, 2011 , vol. 15, # 1 p. 258 - 265

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Citation Number: 3

Abstract

A chemo-enzymatic method for production of β-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 ...