Synthesis of 12-Deuterated and Tritiated Deoxoartemisinins

Mankil      Jung; Kyunghoon      Lee

doi:10.2174/1573406053175319

Abstract

The synthesis of C-12 deuterated and tritiated deoxoartemisinins is described. Tritiated deoxoartemisinin which could be incubated with the protein of Plasmodium falciparum for binding mechanism study was obtained by direct reduction of the carbonyl group of artemisinin using NaBT4 and BF3×Et2O in dried THF.

Keywords: sodium borohydride, deuterium labeling, tritium labeling, malaria, artemisinin, deoxoartemisinin

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Medicinal Chemistry

Title: Synthesis of 12-Deuterated and Tritiated Deoxoartemisinins

Volume: 1 Issue: 2

Author(s): Mankil Jung and Kyunghoon Lee

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Keywords: sodium borohydride, deuterium labeling, tritium labeling, malaria, artemisinin, deoxoartemisinin

Abstract: The synthesis of C-12 deuterated and tritiated deoxoartemisinins is described. Tritiated deoxoartemisinin which could be incubated with the protein of Plasmodium falciparum for binding mechanism study was obtained by direct reduction of the carbonyl group of artemisinin using NaBT4 and BF3×Et2O in dried THF.

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Jung Mankil and Lee Kyunghoon, Synthesis of 12-Deuterated and Tritiated Deoxoartemisinins, Medicinal Chemistry 2005; 1 (2) . https://dx.doi.org/10.2174/1573406053175319