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O O
O O
O
O
O
O
OCH
2
COOH
O(CH
2
)
n
COOH
O
130
131
O O
O O
O
O
O
O
H
C
(CH
2
)
n
COOH
O
(CH
2
)
n
R
OCH
2
COOH
132
Artelinic acid
133
Structure 5-12
dihydroartemisinin, quickly subsides. Hence, the synthesis of stable, water-soluble
qinghaosu derivatives is an important research program.
5.5.2.1 Qinghaosu Derivatives Containing the Carboxyl Group
Because artemether has greater stability than artesunate, it was supposed that the
replacement of the ester linkage by the ether linkage in the artesunate molecule
20
Ester
OO
OO
O
O
HO
O
O
H
H
RO
O
O
23
Ester
134
COOH
OO
O
135
H
HO
O
O
O
O
OH
OH
Scheme 5-18
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