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Synthesis of Two Metabolites of the Antiarrythmicum Amiodarone

✍ Scribed by Barbara Wendt; Huy Riem Ha; Manfred Hesse

Publisher
John Wiley and Sons
Year
2002
Tongue
German
Weight
148 KB
Volume
85
Category
Article
ISSN
0018-019X

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✦ Synopsis

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). 1 H-and 13 C-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.

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