Chemistry Reference
In-Depth Information
Glafenine [3820-67-5], analgesic, anti-inflammatory, 125.
Isatoic anhydride, prepared
from o-aminobenzoic acid 122 and phosgene, has been used as a starting material
in the synthesis of Glafenine [94, 95].
OH
O
O
O
O
COOH
COCl
2
O
124
O
O
O
PhCl, 20°C,
then 105°C
N
H
O
NH
2
NH
2
122
123
124
O
O
OH
OH
NH
125
Glafenine
Cl
N
Gliclazide [21187-98], antidiabetic, 129. 4-Toluenesulfonyl isocyanate (PTSI) 127 is
an interesting, highly reactive isocyanate, which has found several valuable appli-
cations [96]. One of these applications is in the synthesis of the hypoglicemic API
Gliclazide.
O
O
O
O
O
S
S
N
NCO
N
H
N
H
H
2
N
N
129
126
127
Gliclazide
COCl
2
BuNCO
PhCl
O
O
S
NH
2
128
The mechanism of the catalyzed synthesis of 4-toluenesulfonyl isocyanate (PTSI)
