Centre National De La Recherche Scientifique

Emmanuel Gras

Pierre Potier

Claude Thal

Catherine Guillou

Jean-Luc Beunard

The invention relates to a method for the synthesis of galanthamine, the derivatives and analogues thereof of formula (1) where R=a hydrogen atom, R=a hydroxy group, Rand Rtogether form &#x2550;O, R, R, and Rindependently=a hydrogen atom, a hydroxy group or a (C-C)alkoxy group, R&#x2550;H, (C-C)alkyl, (CH)NRR, or &#x2014;(CH)NRRRwhere n=1 to 12, Z=two hydrogen atoms, or an oxygen atom and X=an oxygen, sulphur or nitrogen atom, or a &#x2014;SO, &#x2014;SO, or &#x2014;NRgroup where Ris as defined above or is an amine protecting group.

Total synthesis of galanthamine, analogues and derivatives thereof

The invention relates to a method for the synthesis of galanthamifle, the derivatives and analogues thereof of formula (1) where R=a hydrogen atom. R=a hydroxy group, Rand Rtogether form &#x2550;O, R, R, and Rindependently=a hydrogen atom, a hydroxy group or a (C&#x2013;C)alkoxy group, R&#x2550;H, (C&#x2013;C)alkyl, (CH)NRR, or &#x2014;(CH)N'RRRwhere n=1 to 12, Z=two hydrogen atoms, or an oxygen atom and X=an oxygen, sulphur or nitrogen atom, or a &#x2014;SO, &#x2014;SO, or &#x2014;NRgroup where Ris as defined above or is an amine protecting group 

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Rochefort, France

Emmanuel Gras