Effective Synthesis of 1β-Acyl Glucuronides by Selective Acylation
2005-06-23T00:00:00Z (GMT) by
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 1β-acylation of allyl glucuronate with carboxylic acids catalyzed by HATU and then mild deprotection through treatment with Pd(PPh<sub>3</sub>)<sub>4</sub> and morpholine. The method is effective for a range of aryl and alkyl carboxylic acids, including important drugs.