- Product Name
- CasNo
- MF
- MW
- Content
- Appearance
- Packing
- Apply
- Nintedanib Ethanesulfonate Salt
- 656247-18-6
- C31H33N5O4.C2H6O3S
- 649.768
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nintedanib
ethanesulfonic acid
![methyl (3Z)-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate ethanesulfonate salt](/upload/2024/12/b05b41a1-ad13-42e3-9b38-81a2039692b3.png)
methyl (3Z)-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate ethanesulfonate salt
| Conditions | Yield |
|---|---|
|
In
methanol;
for 4h;
Reflux;
|
100% |
|
In
methanol; water;
at 60 ℃;
|
97.3% |
|
In
methanol; water; isopropyl alcohol;
at 0 - 65 ℃;
for 1h;
|
95% |
|
In
methanol; water;
at 60 - 70 ℃;
for 0.5h;
Temperature;
Large scale;
|
95.2% |
|
In
methanol;
at 50 - 55 ℃;
for 0.5h;
Temperature;
Concentration;
|
91.27% |
|
In
ethanol; water;
at 50 ℃;
|
89.7% |
|
In
methanol; water;
at 60 ℃;
|
89% |
|
In
methanol; water;
at 50 ℃;
|
87.6% |
|
In
methanol; water;
at 60 - 65 ℃;
|
80% |
|
In
methanol; water;
at 50 ℃;
|
|
|
In
dichloromethane;
at 10 ℃;
for 5h;
Large scale;
|
|
|
In
methanol;
at 40 - 50 ℃;
Temperature;
|
|
|
In
methanol; water; isopropyl alcohol;
at 0 - 60 ℃;
for 2h;
|
7 g |
|
In
methanol; dichloromethane;
at 20 - 30 ℃;
for 16h;
|
2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester
methyl (3Z)-3-[({4-[N-methyl-2-(4-methylpiperazin-1-yl)acetamido]phenyl}amino)(phenyl)methylidene]-2-oxo-2,3-dihydro-1H-indole-6-carboxylate ethanesulfonate salt
| Conditions | Yield |
|---|---|
|
Multi-step reaction with 5 steps
1: toluene; cyclohexane / 6 h / 80 - 90 °C / Inert atmosphere
2: acetic anhydride / toluene / 4 h / Reflux
3: methanol; potassium hydroxide / 3 h / Reflux
4: methanol / N,N-dimethyl-formamide / 5 h / Reflux
5: methanol / 4 h / Reflux
With
methanol; acetic anhydride; potassium hydroxide;
In
methanol; cyclohexane; N,N-dimethyl-formamide; toluene;
|
|
|
Multi-step reaction with 5 steps
1: SMO-powder / isopropyl alcohol / 5 h / -10 - -5 °C
2: pyridine / 1.5 h / 0 - 80 °C
3: methanol; N,N-dimethyl-formamide / 12 h / 60 - 65 °C
4: N,N-dimethyl-formamide / 45 - 50 °C
5: methanol; water / 60 - 65 °C
With
pyridine;
In
methanol; water; N,N-dimethyl-formamide; isopropyl alcohol;
|
|
|
Multi-step reaction with 5 steps
1.1: sodium methylate / isopropyl alcohol / 0.25 h
1.2: 5 h / -10 - -5 °C
2.1: pyridine / 0.01 h / 0 - 5 °C
3.1: methanol; N,N-dimethyl-formamide / 12 h / 60 - 65 °C
4.1: N,N-dimethyl-formamide / 45 - 50 °C
5.1: isopropyl alcohol; methanol; water / 1 h / 0 - 65 °C
With
sodium methylate;
In
pyridine; methanol; water; N,N-dimethyl-formamide; isopropyl alcohol;
|
|
|
Multi-step reaction with 4 steps
1.1: toluene / 18 h / 115 - 118 °C
2.1: toluene / Reflux
3.1: methanol; N,N-dimethyl-formamide / Reflux
3.2: Reflux
4.1: methanol; water / 60 °C
In
methanol; water; N,N-dimethyl-formamide; toluene;
|
|
|
Multi-step reaction with 4 steps
1.1: 3 h / 130 °C / Large scale
2.1: acetic anhydride / toluene / 6 h / 120 - 130 °C / Large scale
3.1: methanol / N,N-dimethyl-formamide / 4 h / 75 °C / Large scale
3.2: Large scale
4.1: water; methanol / 0.5 h / 60 - 70 °C / Large scale
With
methanol; acetic anhydride;
In
methanol; water; N,N-dimethyl-formamide; toluene;
|
|
|
Multi-step reaction with 4 steps
1: dmap / toluene / 7 h / 104 - 110 °C
2: N,N-dimethyl-formamide / 10 h / 60 - 65 °C
3: methanol; potassium hydroxide / 2 h / 50 - 55 °C
4: methanol / 40 - 50 °C
With
methanol; dmap; potassium hydroxide;
In
methanol; N,N-dimethyl-formamide; toluene;
|
nintedanib
ethanesulfonic acid
2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester
methyl 1-(2-chloroacetyl)-2-oxoindoline-6-carboxylate
nintedanib