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CAS No.: | 656247-17-5 |
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Name: | Nintedanib |
Article Data: | 30 |
Molecular Structure: | |
Formula: | C31H33N5O4 |
Molecular Weight: | 539.634 |
Synonyms: | Vargatef; |
EINECS: | 1592732-453-0 |
Density: | 1.284g/cm3 |
Boiling Point: | 742.199°C at 760 mmHg |
Flash Point: | 402.667°C |
PSA: | 94.22000 |
LogP: | 3.70270 |
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
nintedanib
Conditions | Yield |
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With sodium hydrogencarbonate In water; ethyl acetate at 40℃; for 1h; | 98.7% |
With sodium carbonate In water pH=9; Solvent; pH-value; | 20 g |
N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine
(E)-1-acetyl-3-(methoxy-phenyl-methylene)-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester
nintedanib
Conditions | Yield |
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Stage #1: N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine; (E)-1-acetyl-3-(methoxy-phenyl-methylene)-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester With methanol In N,N-dimethyl-formamide at 75℃; for 4h; Large scale; Stage #2: With methanol; potassium hydroxide In N,N-dimethyl-formamide Temperature; Large scale; | 94.6% |
Stage #1: N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine; (E)-1-acetyl-3-(methoxy-phenyl-methylene)-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester In methanol for 5h; Reflux; Stage #2: With potassium hydroxide In methanol at 20 - 70℃; for 0.5h; Concentration; Reagent/catalyst; Temperature; Solvent; | 90% |
Stage #1: N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine; (E)-1-acetyl-3-(methoxy-phenyl-methylene)-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester In methanol; N,N-dimethyl-formamide Reflux; Stage #2: With piperidine In methanol; N,N-dimethyl-formamide Reflux; | 88% |
Stage #1: N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine; (E)-1-acetyl-3-(methoxy-phenyl-methylene)-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester In methanol for 5h; Reflux; Stage #2: With potassium hydroxide In methanol | 84% |
Stage #1: N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine; (E)-1-acetyl-3-(methoxy-phenyl-methylene)-2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester In N,N-dimethyl-formamide at 80℃; for 1h; Stage #2: With piperidine In N,N-dimethyl-formamide at 20℃; for 2h; | 77% |
Conditions | Yield |
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In N,N-dimethyl-formamide at 45 - 50℃; | 93.74% |
Conditions | Yield |
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In N,N-dimethyl-formamide at 45 - 50℃; | 93.74% |
Conditions | Yield |
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In toluene at 65℃; for 4h; Solvent; Temperature; | 93% |
N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine
nintedanib
Conditions | Yield |
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With sodium hydrogencarbonate In ethanol for 2h; Reflux; | 92.7% |
N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine
nintedanib
Conditions | Yield |
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With pyrrolidine In methanol at 25 - 50℃; for 6h; | 91.37% |
nintedanib
Conditions | Yield |
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With methanol; potassium hydroxide at 20℃; Reagent/catalyst; Large scale; | 91.3% |
With methanol; potassium hydroxide at 50 - 55℃; for 2h; Temperature; |
N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine
(E)-methyl 3-(methoxy(phenyl)methylene)-2-indolone-6-carboxylic acid methyl ester
nintedanib
Conditions | Yield |
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In methanol for 8h; Reflux; | 90.8% |
benzoic acid methyl ester
N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine
2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester
nintedanib
Conditions | Yield |
---|---|
Stage #1: benzoic acid methyl ester; 2-oxo-2,3-dihydro-1H-indole-6-carboxylic acid methyl ester With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 3h; Stage #2: N-[(4-methyl-piperazin-1-yl)methylcarbonyl]-N-methyl-p-phenylendiamine In N,N-dimethyl-formamide at 20℃; for 4h; | 89.7% |