2-Hydroxyestradiol 2- and 3-monoglucuronides (X, V) were prepared from the suitably protected catechol estrogen derivatives employing Koenigs-Knorr reaction as shown in Chart 1. These synthetic glucuronides underwent readily hydrolysis to furnish 2-hydroxyestradiol and free glucuronic acid when incubated with beef-liver β-glucuronidase preparation.
