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Synthesis of 14-[2H]arteether, an experimental antmalarial drug

✍ Scribed by Yulin Hu; Herman Ziffer

Book ID
102375790
Publisher
John Wiley and Sons
Year
1991
Tongue
French
Weight
265 KB
Volume
29
Category
Article
ISSN
0022-2135

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✦ Synopsis

Abstract

A reaction sequence employing a fungus mediated oxidation of arteether, an experimental antimalarial drug, was used to introduce a hydroxyl group on C‐14. The hydroxyl group was replaced by a deuterium by preparing the tosylate and reductively cleaving it with sodium borodeuteride in DMSO. A reaction sequence to introduce a second label was also demonstrated it involved oxidation of the alcohol, with catalytic quantities of tetra‐n‐propylammonium perruthenate, followed by reduction with sodium borodeuteride to regenerate the alcohol. Use of both reactions sequences yield arteether containing two deuterium.

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