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PROCESS FOR SYNTHESIS OF GALANTAMINE AND ITS ANALOGUES |
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Principal Investigator: Claude THAL
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TECHNICAL DESCRIPTION
The present invention concerns a process for the synthesis of galanthamine analogues and derivatives thereof. The described synthesis is the shortest and most efficient non biomimetic total synthesis of galanthamine to date. (-)-Galanthamine, a tertiary alkaloid isolated from Amaryllidaceae, is a centrally-acting competitive and reversible inhibitor of acetylcholinesterase which enhances cognitive functions of Alzheimer's patients. This drug is the most recently approved acetylcholinesterase inhibitor for use. However, the botanical supplies of galanthamine are insufficient for its clinical uses. The research team that developed this invention works on new acetylcholinesterase inhibitors. The invention also describes synthetic intermediates useful for structure activity relationships studies in the galanthamine series.
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