The invention relates to a process for the preparation of 2-arylethylamine derivates having an alkyl substituent in the 1-position, of the formula (I)
aryl-CHR
1
—CR
2
(NR
3
R
4
)—(CHR
5
R
6
)
n
—CHR
7
R
8
(I)
by reaction of aromatic olefins of the general formulae (Ila-c)
aryl-CHR
1
—CHR
2
—(CR
5
R
6
)
a
—CR
5
═CR
6
—(CR
5
R
6
)
b
CHR
7
R
8
(IIa)
aryl-CHR
1
—CR
2
═CR
5
—(CR
5
R
6
)
c
—CHR
7
R
8
(IIb)
aryl-CHR
1
—CHR
2
—(CR
5
CR
6
)
c
—CR
5
═CR
7
CR
8
(IIc)
with amines of the general formula (III)
R
3
R
4
NH
in the presence of a base.
本发明涉及一种 2-芳基
乙胺衍
生物的制备方法,该衍
生物在 1 位具有烷基取代基,其式为 (I)
芳基-CHR
1
-CR
2
(NR
3
R
4
)-(CHR
5
R
6
)
n
-CHR
7
R
8
(I)
通过与通式(Ila-c)的芳香族烯烃反应
芳基-CHR
1
-CHR
2
-(CR
5
R
6
)
a
-CR
5
═CR
6
-(CR
5
R
6
)
b
CHR
7
R
8
(IIa)
芳基-CHR
1
-CR
2
═CR
5
-(CR
5
R
6
)
c
-CHR
7
R
8
(IIb)
芳基-CHR
1
-CHR
2
-(CR
5
CR
6
)
c
-CR
5
═CR
7
CR
8
(IIc)
与通式(III)的胺
R
3
R
4
NH
在有碱存在的情况下。