Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent
A practical enzymic approach for acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H ‐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 rend...
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crwiley:10.1111/j.1470-8744.1999.tb00554.x 2024-06-23T07:47:40+00:00 Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent Mahmoudian, Mahmoud Eaddy, John Dawson, Mike 1999 http://dx.doi.org/10.1111/j.1470-8744.1999.tb00554.x https://iubmb.onlinelibrary.wiley.com/doi/pdf/10.1111/j.1470-8744.1999.tb00554.x en eng Wiley http://onlinelibrary.wiley.com/termsAndConditions#vor Biotechnology and Applied Biochemistry volume 29, issue 3, page 229-233 ISSN 0885-4513 1470-8744 journal-article 1999 crwiley https://doi.org/10.1111/j.1470-8744.1999.tb00554.x 2024-06-11T04:50:37Z A practical enzymic approach for acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H ‐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%. Article in Journal/Newspaper Antarc* Antarctica Wiley Online Library Biotechnology and Applied Biochemistry 29 3 229 233 |
institution |
Open Polar |
collection |
Wiley Online Library |
op_collection_id |
crwiley |
language |
English |
description |
A practical enzymic approach for acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H ‐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%. |
format |
Article in Journal/Newspaper |
author |
Mahmoudian, Mahmoud Eaddy, John Dawson, Mike |
spellingShingle |
Mahmoudian, Mahmoud Eaddy, John Dawson, Mike Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent |
author_facet |
Mahmoudian, Mahmoud Eaddy, John Dawson, Mike |
author_sort |
Mahmoudian, Mahmoud |
title |
Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent |
title_short |
Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent |
title_full |
Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent |
title_fullStr |
Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent |
title_full_unstemmed |
Enzymic acylation of 506U78 (2‐amino‐9‐β‐D‐arabinofuranosyl‐6‐methoxy‐9 H‐purine), a powerful new anti‐leukaemic agent |
title_sort |
enzymic acylation of 506u78 (2‐amino‐9‐β‐d‐arabinofuranosyl‐6‐methoxy‐9 h‐purine), a powerful new anti‐leukaemic agent |
publisher |
Wiley |
publishDate |
1999 |
url |
http://dx.doi.org/10.1111/j.1470-8744.1999.tb00554.x https://iubmb.onlinelibrary.wiley.com/doi/pdf/10.1111/j.1470-8744.1999.tb00554.x |
genre |
Antarc* Antarctica |
genre_facet |
Antarc* Antarctica |
op_source |
Biotechnology and Applied Biochemistry volume 29, issue 3, page 229-233 ISSN 0885-4513 1470-8744 |
op_rights |
http://onlinelibrary.wiley.com/termsAndConditions#vor |
op_doi |
https://doi.org/10.1111/j.1470-8744.1999.tb00554.x |
container_title |
Biotechnology and Applied Biochemistry |
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29 |
container_issue |
3 |
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229 |
op_container_end_page |
233 |
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1802651808812761088 |