Chemistry Reference
In-Depth Information
N
O
H
N
T
O
H
N
T
O
N
3
O
O
T
t
BuPh
2
SiO
O
O
60
t
BuPh
2
SiO
61
I
t
BuPh
2
SiO
O
H
T
59
I
O
O
H
N
N
O
N
T
O
NH
t
BuPh
2
SiO
62
T =
63
N
O
t
BuPh
2
SiO
T
t
Bu
T
HO
HO
t
Bu
O
O
CuSO
4
Na ascorbate
t
BuOH/H
2
O,
rt, overnight
HSi
HSi
+
N
N
t
Bu
t
Bu
N
3
O
N
O
6
6
5
6
6
77%
Synthesis of 3
-and6
- triazolo-thymidine derivatives suitable for iodination
SCHEME 7.13
and fluorination.
t
Bu
t
Bu
T
N
3
CuSO
4
Na ascorbate
tBuOH/H
2
O, 100 °C
O
HSi
HSi
N
N
+
T
N
t
Bu
t
Bu
O
O
O
HO
99 %
HO
6
6
8
6
9
K[
18
F
]F
-
, K
222
Cl
P
DMSO, AcOH
60 °C, 15', 34 %
NC(CH
2
)
2
O
N(iPr)
2
iPr
2
EtN, THF, 45', 60 %
t
Bu
t
Bu
18
F
Si
HSi
N
N
N
N
T
T
t
Bu
N
t
Bu
N
O
O
O
O
71
70
O
HO
NC
P
O
N(iPr)
2
t
Bu
t
Bu
18
F
Si
HSi
N
N
N
N
T
K[
18
F
]F
-
, K
222
T
N
t
Bu
N
t
Bu
O
O
O
O
DMSO, AcOH
100 °C, 15', 36 %
7
7
3
ODN
ODN
ODN = 5'-d(GACTGACGC)-3'
SCHEME 7.14
18
F-fluorination of 3
-and6
-triazolo-thymidine derivatives.
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