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

被引：5

作者：

Atzrodt, Jens ^{[1
]}

Derdau, Volker ^{[1
]}

Holla, Wolfgang ^{[1
]}

Sandvoss, Martin ^{[1
]}

机构：

[1] Sanofi Aventis Deutschland GmbH, R&D, SCP Disposit Safety & Anim Res DSAR, DD,ICMS, G876, D-65926 Frankfurt, Germany

来源：

ARKIVOC | 2012年

关键词：

Phase II metabolites; glucuronides; acyl glucuronides; sulfates; metabolite analysis; HYDROPHILIC-INTERACTION CHROMATOGRAPHY; WHOLE-CELL BIOTRANSFORMATION; CHEMICAL-SYNTHESIS; 1-BETA-O-ACYL GLUCURONIDES; CONVENIENT SYNTHESIS; ACYL GLUCURONIDES; SGLT INHIBITORS; SAFETY; STRATEGIES; ACID;

D O I：

10.3998/ark.5550190.0013.319

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学];

摘要：

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-acyl-glucuronide 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.

引用

页码：257 / 278

页数：22

共 77 条

[1]

Anomalous Zemplen deacylation reactions of α- and β-D-mannopyranoside derivatives [J].