1609409-53-1

Basic information

• Product Name: ethyl {5-hydroxy-6-oxo-1-[4-(2-oxopiperidin-1-yl)phenyl]-1,2,3,6-tetrahydropyridin-4-yl}(oxo)acetate
• Synonyms: ethyl {5-hydroxy-6-oxo-1-[4-(2-oxopiperidin-1-yl)phenyl]-1,2,3,6-tetrahydropyridin-4-yl}(oxo)acetate
• CAS NO: 1609409-53-1
• Molecular Weight: 386.404
• Mol File: 1609409-53-1.mol

Chemical Properties

• CAS DataBase Reference: ethyl {5-hydroxy-6-oxo-1-[4-(2-oxopiperidin-1-yl)phenyl]-1,2,3,6-tetrahydropyridin-4-yl}(oxo)acetate(CAS DataBase Reference)
• NIST Chemistry Reference: ethyl {5-hydroxy-6-oxo-1-[4-(2-oxopiperidin-1-yl)phenyl]-1,2,3,6-tetrahydropyridin-4-yl}(oxo)acetate(1609409-53-1)
• EPA Substance Registry System: ethyl {5-hydroxy-6-oxo-1-[4-(2-oxopiperidin-1-yl)phenyl]-1,2,3,6-tetrahydropyridin-4-yl}(oxo)acetate(1609409-53-1)

Safety Data

• Hazardous Substances Data: 1609409-53-1(Hazardous Substances Data)

Upstream product

• 454183-28-9 3-(4-nitrophenylamino)propionic acid ethyl ester 
• 100-01-6 4-nitro-aniline 
• 545445-44-1 5,6?dihydro?3?(4?morpholinyl)?1?[4?(2?oxo?1?piperidinyl)phenyl]?2(1H)?pyridone 
• 4755-77-5 Ethyl oxalyl chloride 
• 1609409-55-3 3-ethoxy-1-[4-(2-oxopiperidin-1-yl)phenyl]-5,6-dihydropyridin-2(1H)-one 
• 64-17-5 ethanol 
• 1609409-54-2 {5-hydroxy-6-oxo-1-[4-(2-oxopiperidin-1-yl)phenyl]-1,2,3,6-tetrahydropyridin-4-yl}(oxo)acetic acid 

Downstream Products

• 503614-91-3 1-(4-methoxy-phenyl)-7-oxo-6-[4-(2-oxo-piperidin-1-yl)-phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid ethyl ester 
• 503614-92-4 1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxylic acid 

Relevant articles and documents

A method for synthesizing [...]

The invention discloses a synthetic method of novel Apixaban. The method comprises the following steps: (i) hydrolyzing an Apixaban precursor compound (II) to obtain a carboxylic acid product; and (ii) mixing the carboxylic acid product obtained in the step (i) with ethyl chloroformate, reacting in the presence of diisopropylethylamine at the temperature of 0-5 DEG C for 3-5 hours; then introducing ammonia gas and reacting to obtain an ammonolysis product, namely, Apixaban. By adopting the method for preparing Apixaban by using the Apixaban precursor compound (II), the yield of Apixaban can be up to 93 percent. In the entire synthesis route, the minimum yield in each step is over 76 percent at least, and the total yield is about 33 percent. In the entire process, the use of precious catalysts or auxiliary reagents is avoided.

PROCESS FOR THE SYNTHESIS OF APIXABAN

The present invention relates to the Process for the preparation of Apixaban and novel intermediates useful in the synthesis of Apixaban (I).