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We have summarized methods for the preparation of phase II metabolites which have proven to be successful in our laboratory for the synthesis of selected O-glucuronides and sulfates of recent drug development candidates. The syntheses of the O-glucuronides AVE0897 O-acylglucuronide 7, AVE2268 O-glucuronide 12, SAR7226 O-glucuronide 21 and the preparation of the sulfates 28 of AVE2268 and MDL107292 33 are described in detail. Analytical aspects related to phase II metabolites and specific chromatographic methods of very polar compounds are discussed.

The synthesis of selected phase II metabolites – Ο-glucuronides and sulfates of drug development candidates