Glucuronidation of steroidal alcohols using iodosugar and imidate donors |
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Authors: | Harding John R King Clare D Perrie Jennifer A Sinnott Deborah Stachulski Andrew V |
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Affiliation: | AstraZeneca UK Ltd., Drug Metabolism and Pharmacokinetics Department, Mereside, Cheshire, UK. |
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Abstract: | We report a study of the glucuronidation of a number of important steroidal secondary alcohols. The alcohols studied are androsterone 7, epiandrosterone 8, 17-acetoxy-androstane-3alpha,17beta-diol 9, 11alpha-hydroxyprogesterone 10, and 3-benzoylestradiol 11. These were first glucuronidated using the Schmidt trichloroacetimidate method with variations in acyl substituent (viz. derivatives 2 and 3), Lewis acid catalyst and order of addition. The results are contrasted with those obtained using our recently described glycosyl iodide donor 4, catalysed either by N-iodosuccinimide (NIS) or various metal salts. |
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