(Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate synthesis
- Product Name:(Z)-methyl 3-((4-(N-methyl-2-(4-methylpiperazin-1-yl)acetamido)phenylamino)(phenyl)methylene)-2-oxoindoline-6-carboxylate
- CAS Number:1160294-26-7
- Molecular formula:C31H33N5O4
- Molecular Weight:539.62
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Yield: 91.6%
Reaction Conditions:
in methanol;N,N-dimethyl-formamide for 8 h;Reflux;Large scale;
Steps:
4 Synthesis of nintedanib:
12 kg of a compound of formula (I) and 3-[methoxy(phenyl)methylene]-2-oxoindolin-6-formic acid methyl ester 13.4 kg. It was added to a mixed solution of 21 L of N,N-dimethylformamide and 84 L of anhydrous methanol, and heated under reflux. After 8 hours of reaction, the temperature of the reaction solution was lowered to 20 ° C or lower and stirred for 4 hours. The filter cake was shaken, the filter cake was washed with methanol, and dried to obtain 21.2 kg of a yellow solid with a molar yield of 91.6%. The purity by HPLC detection was 99.93%, the maximum unknown single impurity: 0.04%, and the impurity 2: 0.03% (see Figure 3 for the HPLC chart).
References:
Jiangsu Haosen Pharmaceutical Group Co., Ltd.;You Junhui;Cao Jin;Cao Yinfei;Zhang Xiaozhou;Zhang Xiaobing CN110746378, 2020, A Location in patent:Paragraph 0036; 0039
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109-01-3
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