Biomedical Engineering Reference
In-Depth Information
SCHEME 5.24
Heck-aza-Michael domino sequence.
TABLE 5.15 Representative Sultam Analogs 63 Obtained from the Reaction Sequence
Shown in 5.24
Entry
R
1
R
2
R
3
Yield (%)
1
H
i
-Pr
OMe
63a
,44
2
H
c
-Hex
Me
63b
,29
3
H
Ph
OH
63c
,35
4
H
3-OMe-Ph
OEt
63d
,22
5
F
Bn
OMe
63e
,75
6
F
n
-Oct
OEt
63f
,54
7
F
c
-Pent
OEt
63g
,87
8
F
t
-Bu
OEt
63h
,46
9
CF
3
i
-Pr
OEt
63i
,50
10
CF
3
c
-Hex
OMe
63j
,51
11
CF
3
c
-Hex
OH
63k
,46
12
CF
3
Bn
OH
63l
,44
SCHEME 5.25
Double-Heck coupling derived sultams
65
.