4.2 Bioorthogonal Chemistry
103
Table 4.1
Examples of pyrazoline and pyrazole-containing APIs that have previously been synthesised using NI cycloaddition
Entry Structure
Source
Target
References
1
N
N
N
CONH
2
OMe
O
N
O
Bristol-Meyers-Squibb
Blood coagulation factor X
a
[14]
2
NH
N
N
HO
2 C
Me
H
H
CO
2 H
Pfizer
AMPA receptor
[15]
3
CO
2 H
OH OH
N N
NH
O
Me
i
Pr
F
Pfizer
HMG-CoA reductase
[16]
(continued)
103
Table 4.1
Examples of pyrazoline and pyrazole-containing APIs that have previously been synthesised using NI cycloaddition
Entry Structure
Source
Target
References
1
N
N
N
CONH
2
OMe
O
N
O
Bristol-Meyers-Squibb
Blood coagulation factor X
a
[14]
2
NH
N
N
HO
2 C
Me
H
H
CO
2 H
Pfizer
AMPA receptor
[15]
3
CO
2 H
OH OH
N N
NH
O
Me
i
Pr
F
Pfizer
HMG-CoA reductase
[16]
(continued)