Sulphonyl compounds for use as linkers in solid phase and combinatorial synthesis
申请人:Fujisawa Pharmaceutical Co. Ltd.
公开号:US20010012901A1
公开(公告)日:2001-08-09
The present invention relates to a linker shown by the following formula (I):
X—S0
2
—R
1
—(A)
m
—R
2
(I)
wherein R
1
is a group of the formula (A):
1
[wherein
R
3
, R
4
and R
5
are the same or different hydrogen, etc], etc,
R
2
is a group which can form a chemical bond to a resin which may be protected by a conventional protective group,
A is lower alkylene, etc,
X is a leaving group, and
m is an integer of 0 or 1,
with proviso that A is (C
2
-C
6
)alkylene, and m is an integer of 1,
when R
1
is a group of the formula (A).
本发明涉及一种由以下式(I)所示的连接剂:X—S02—R1—(A)m—R2(I)其中,R1是式(A)的基团:1 [其中R3,R4和R5相同或不同,为氢等等],等等,R2是可以形成与可能由传统保护基保护的树脂的化学键的基团,A是低级烷基等,X是离去基,m是0或1的整数,条件是当R1是式(A)的基团时,A是(C2-C6)烷基,m是1的整数。