申请人:Thal Claude
公开号:US20050065338A1
公开(公告)日:2005-03-24
The invention relates to a method for the synthesis of galanthamine, the derivatives and analogues thereof of formula (1) where R
1
=a hydrogen atom. R
2
=a hydroxy group, R
1
and R
2
together form =0, R
3
, R
4
, and R
5
independently=a hydrogen atom, a hydroxy group or a (C
1
-C
2
) alkoxy group, R
6
-11 , (C
1
-C
12
) alkyl, (CH
2
)
n
NR
7
R
8
, or —(CH
2
)
n
N′R
7
R
8
R
9
where n−1 to 12 Z=two hydrogen atoms, or an oxygen atom and X=an oxygen, sulphur or nitrogen atom, or a —SO, —SO
2
, or —NR
6
group where R
6
is as defined above or is an amine protecting group.
本发明涉及一种合成加兰他明及其衍生物和类似物的方法,其化学式为(1),其中R1为氢原子,R2为羟基,R1和R2组成=0,R3、R4和R5独立地为氢原子、羟基或(C1-C2)烷氧基,R6-11为(C1-C12)烷基、(CH2)nNR7R8或—(CH2)nN′R7R8R9,其中n为1到12,Z为两个氢原子或一个氧原子,X为氧、硫或氮原子,或—SO、—SO2或—NR6基团,其中R6如上所定义或为氨基保护基团。