Effective synthesis of 1beta-acyl glucuronides by selective acylation |
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Authors: | Perrie Jennifer A Harding John R Holt David W Johnston Atholl Meath Paul Stachulski Andrew V |
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Institution: | The Robert Robinson Laboratories, Department of Chemistry, University of Liverpool, UK. |
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Abstract: | reaction: see text] Acyl glucuronides are vital metabolites for many carboxylic acid containing drugs. We report an efficient new method for the chemical synthesis of these molecules by selective 1beta-acylation of allyl glucuronate with carboxylic acids catalyzed by HATU and then mild deprotection through treatment with Pd(PPh(3))(4) and morpholine. The method is effective for a range of aryl and alkyl carboxylic acids, including important drugs. |
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