Product Name: Apixaban
Synonyms: Apixaban;Apixaban, BMS 562247-01;1H-Pyrazolo[3,4-c]pyridine-3-carboxamide, 4,5,6,7-tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-;1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide;BMS562247;BMS 562247-01;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 aMide;1-(4-Methoxyphenyl)-7-oxo-6-[4-(2-oxopiperidin-1-yl)phenyl]-4, 5-dihydropyrazolo[3,4-c]pyridine-3-carboxaMide
CAS: 503612-47-3
MF: C25H25N5O4
MW: 459.5
EINECS: 639-684-6
Boiling point: 770.5±60.0 °C

Description:

Eliquis (apixaban), a direct inhibitor of factor Xa (FXa), was approved by the European Commission on May 18, 2011 for prevention of venous thromboembolic events (VTE) in adult patients who have undergone elective hip or knee replacement surgery. The discovery of apixaban was the culmination of a succession of novel and innovative medicinal chemistry discoveries starting with the identification of nonpeptide leads, rational drug design using computer-aided and X-ray crystallographic information, and the building of drug-like properties through the systematic replacement of basic groups with neutral moieties. Apixaban arose from modifications to razaxaban by constraining a pyrazole amide to form a bicyclic pyrazolo-pyridinone scaffold.
Optimization of the P1 group resulted in the identification of the nonbasic methoxy phenyl group, while a P4 piperidinone improved the balance of potency and pharmacokinetics with low Vdss. The synthesis of apixaban begins with the generation of a hydrazone of 4-methoxyaniline which is then used in a 3+2 cycloaddition with a dihydropiperidinone to form a bicyclic pyrazolo-pyridinone scaffold. The distal piperidinone group is installed using an Ullmann coupling reaction followed by aminolysis of an ethyl ester on the pyrazole ring to complete the synthesis of apixaban.

Usage:

Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.

1. Rich experience: Our company is a professional production leading factory in China in pharmaceutical area of many years. 

2. Top quality: High quality guaranteed, once any problem is found, the package would be reshipped for you .

3. Security Shipping: Shipping by express (FedEx,UPS,DHL,EMS), by air. The most professional forwarder would be recommanded for you.

4. Fast delivery: We have stock, so we can delivery quickly once payment is received.

5. Quality service: We will give you warm after-sale service,if any question we will reply you within 24 hours.

6. Competitive prices: A discount would be given when you make a large order.

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Hubei Yuanmeng Biological Technology Co., Ltd., which is located in Wuhan, China. We are specializing in the exportation of APIs, and plant extracts ect.

Our products has been exported to America, Australia, Brazil, the Europe, Middle East and other areas in the world. We have established close and stable cooperative relationships with over 200 domestic pharmaceutical and chemical enterprises. With high quality and favorable price, we′ re pleased to get your inquiry and we will reply you as soon as possible.

We will continue to forge ahead and strive hard for excellence, keep on exploring and progressing to develop more high-tech products with superior quality, to satisfy increasing demand of the clients, and create more value for our partners!


Contact us!

Hubei Yuanmeng Biological Technology Co., Ltd.
Room 3820, Building 2, Vanke Golden City, Hongshan District, Wuhan, Hubei, China
Fiona Wei / Sales Manager