Biocatalytic preparation of 5-methyluridine (5-MU)

Abstract

The potential of chemo-enzymatic methods to produce active pharmaceutical ingredients (APIs) such as stavudine (d4T) and zidovudine (AZT) has been demostrated during this investigation. The effect of increasing reactor productivity to commercially viable levels, albeit as low substrate solubilities, was also demonstrated. The process also demonstrated the isolation of 5-methyluridine (5-MU) from the biocatalytic reaction and integration into the subsequent chemical steps to produce B-thymidime, a key intermediate in the preparation of antiretrovirals. The current paper discusses how the above challenges were successfully overcome and implemented at 20 L scale.