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- Title
Synthesis of Two Metabolites of the Antiarrythmicum Amiodarone.
- Authors
Wendt, Barbara; Riem Ha, Huy; Hesse, Manfred
- Abstract
The metabolism of the potent antiarrythmic drug amiodarone (AMI; 1) has yet not been fully investigated. Recently, in vitro experiments revealed that in rabbit-liver microsomes, AMI ( 1) and its main metabolite MDEA ( 2) were biotransformed to the hydroxylated derivatives 3′-OH-AMI ( 3) and 3′-OH-MDEA ( 4), respectively. To establish the chemical structure of 3 and 4, we developed a total synthesis of these two metabolites of AMI ( 1). 1H- and 13C-NMR Signal assignment from HSQC and HMBC 2D NMR data of synthesized 4 showed that the proposed structure of metabolite 4 is correct. Even the structure of 3 was found to be correct by comparing its HPLC/MS-MS/MS with the data described earlier.
- Publication
Helvetica Chimica Acta, 2002, Vol 85, Issue 9, p2990
- ISSN
0018-019X
- Publication type
Article
- DOI
10.1002/1522-2675(200209)85:9<2990::AID-HLCA2990>3.0.CO;2-R