Felodipine synthesis
- Product Name:Felodipine
- CAS Number:72509-76-3
- Molecular formula:C18H19Cl2NO4
- Molecular Weight:384.25
626-34-6
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105-45-3
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6334-18-5
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72509-76-3
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Yield:72509-76-3 94.3%
Reaction Conditions:
Stage #1: ethyl 3-aminobut-2-enoate;acetoacetic acid methyl ester;2,3-dichlorobenzylaldehydewith piperidine;pyridine in neat (no solvent) at 75 - 80; for 9 h;
Stage #2: with ethanol for 1 h;Reflux;Reagent/catalyst;Solvent;
Steps:
4 Example 4
20.0-dichlorobenzaldehyde 70.0 g (0.40 mol), β-aminocrotonate ethyl ester in a 500 mL round bottom flask55.8g (0.48mol),62.0 g (0.48 mol) of methyl acetoacetate, followed by 4.5 g (0.053 mol) of piperidine and 4.2 g (0.053 mol) of pyridine.The heating was started slowly and the temperature was raised. The reaction was maintained at 75-80 ° C for 9 h, and 200 g of absolute ethanol was added while heating, and the mixture was heated to reflux for 1 h, and filtered while hot.The mixture was cooled to 15 ° C and stirred for 1 h, and suction filtered. The filter cake was washed with a small amount of dry ethanol and dried to give 145 g of pale yellow solid.Yield: 94.3%, purity 99.1%
References:
CN108840819,2018,A Location in patent:Paragraph 0014; 0040-0042; 0045-0048; 0051-0053
![Butanoic acid, 2-[(2,3-dichlorophenyl)methylene]-3-oxo-, ethyl ester](/CAS/20200119/GIF/94739-24-9.gif)
94739-24-9
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72509-76-3
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175688-78-5
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![Butanoic acid, 2-[(2,3-dichlorophenyl)methylene]-3-oxo-, (1S)-1-[[[(4-methylphenyl)sulfonyl]phenylamino]methyl]-2-[(tetrahydro-2H-pyran-2-yl)oxy]ethyl ester](/CAS/20210305/GIF/1215080-80-0.gif)
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72509-76-3
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