New kilogram-synthesis of the anti-Alzheimer drug (-)-galanthamine

被引:63
作者
Czollner, L
Frantsits, W
Küenburg, B
Hedenig, U
Fröhlich, J
Jordis, U
机构
[1] Vienna Univ Technol, Inst Organ Chem, A-1060 Vienna, Austria
[2] Sanochemia AG, A-2491 Neufeld, Austria
关键词
asymmetric synthesis; phenols; polycyclic heterocyclic compounds;
D O I
10.1016/S0040-4039(98)00294-9
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A concise, scalable synthesis of(-)-galanthamine, a drug being used for the treatment of Alzheimer's disease, is described. The yield of the critical phenolic coupling step was optimized to 45-50%. For the reduction of the aryl bromide, air-activated LiAlH4 was used and racemic narwedine was converted to (-)-narwedine by a second order asymmetric transformation. (C) 1998 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码:2087 / 2088
页数:2
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