Labeled Internal Standards of Glucornic Acid Drug Metabolites

Synthesis of 13C6-glucuronic Acid Drug Metabolites

Authors: Alexander Wong PhD, Peech Reddy PhD, Martha Liu PhD
Presented at AAPS, November 2009

Abstract
Analysis of drugs and metabolites is accomplished via the use of labeled internal standards. However, stable isotope labeling of parent drugs can be synthetically challenging. Since glucuronides are primary metabolites of many drugs, one alternative would be the incorporation of the stable isotope into the glucuronic acid moiety. To this end, a ¹³C₆-glucuronic acid sugar donor was synthesized and used in the synthesis of ethynylestradiol and AZT ¹³C₆-glucuronides.

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