| Autor: |
Mahmoudian M; Bioprocessing Unit, Glaxo Wellcome Research and Development, Medicines Research Centre, Gunnels Wood Road, Stevenage, Herts., SG1 2NY, U.K., Eaddy J, Dawson M |
| Jazyk: |
angličtina |
| Zdroj: |
Biotechnology and applied biochemistry [Biotechnol Appl Biochem] 1999 Jun; Vol. 29 (3), pp. 229-33. |
| Abstrakt: |
A practical enzymic approach for acylation of 506U78 (2-amino-9-beta-D-arabinofuranosyl-6-methoxy -9H-purine), a powerful anti-leukaemic agent, is described. Novozyme-435, an immobilized preparation of Candida antarctica lipase, was used to acylate 506U78 regioselectively at the 5'-position. This rendered the compound more soluble and bioavailable. Vinyl acetate was used as the acyl donor and reactions were carried out in anhydrous 1,4-dioxane with up to 100 g/l of substrate input. Bioconversions were optimised to achieve impurity (3'-mono- and di-acetates) levels of less than 0.5%. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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