Deferasirox API

CAS No: 201530-41-8
Appearance: white or off-white powder
Standard: in-house, 99%
Supply Ability: 500kg per month
Shelf Life: Two years
Application: Anti-Anemia 
Payment: T/T, LC or DA
Delivery Time: Ready Stock in Local Warehouse, 1-3 days
Prompt and Secure Shipment
Origin: China
Shipping: DHL, FedEx, TNT, EMS, By Sea, By Air
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Product Introduction

We supply Deferasirox API

We're proud to offer Deferasirox API as a part of our product portfolio. It's a drug used to treat habitual iron load in cases with conditions similar as beta- thalassemia and other blood diseases. Our high- quality API is manufactured according to the strictest norms, icing the utmost chastity and energy. With our product greasepaint, you can trust that you're entering a top- quality product that meets the requirements of your cases. communicate us moment to learn further about our Deferasirox and how it can profit your pharmaceutical operations.

 

What is Deferasirox API?

Deferasirox API, also known as 4-( 3,5- di( 2- hydroxyphenyl)) benzoic acid, is an iron chelating agent product developed by Novartis Pharmaceuticals in Switzerland. It's the first oral iron repellent approved by the US FDA for routine use and has been approved for use in cases progressed ≥ 2 times with habitual iron load caused by blood transfusion. In Europe, it's recommended as a first- line drug for iron load cases with thalassemia over 6 times old. Clinical exploration is presently underway in China; Phase II and III clinical trials and pharmacokinetic studies have shown that it has good safety and tolerability, and can significantly reduce iron cargo on the heart and liver, making it easy for cases to accept. At the same time, it also has pharmacological parcels similar as antifungal parcels( similar as growth of Aspergillus in iron rich surroundings), anti cell proliferation, anti malaria, antioxidant stress damage, and anti cytotoxic induction of cell apoptosis; Deferasirox powder can be used for the treatment of secondary hemochromatosis, delayed skin porphyria, and other conditions.

 

Basic Information

Product Name: Deferasirox

CAS:201530-41-8

MF:C21H15N3O4

MW:373.36

EINECS:685-491-5

MDL No.:MFCD09951804

Purity: 99%+

MOQ: 1kg

Origin: China

Application: Anti-Anemia

Delivery Time: 3-7days

Structural formula:

product-1-1

Melting point: 260-2620C

Boiling point: 672.1 ± 65.0 ° C (Predicted)

Density: 1.40 ± 0.1 g/cm3 (Predicted)

Solubility: soluble in DMSO (10mg/ml)

 

Technical Specification:

Item

Specification

Results

Appearance

White or yellowish powder

Yellowish powder

Solubility

Freely soluble in N,N-dimethylformamide, practically insoluble in water.

Conforms

Identification

IR

The infrared absorption spectrophotometry of sample corresponds to that of reference substance.

Conforms

HPLC

The retention time of the major peak in chromatogram of the sample preparation corresponds to that of the standard preparation, as obtained in assay.

Conforms

Loss on drying

≤ 0.5%

0.12%

Residue on ignition

≤0.1%

0.05%

Heavy metals

≤10ppm

Conforms

Residue Solvents

Methanol

≤3000ppm

Not detected

Xylene

≤2170ppm

Not detected

Ethanol

≤5000ppm

Not detected

Pyridine

≤200ppm

Not detected

Dichloromethane

≤600ppm

Not detected

Acetone

≤5000ppm

3042ppm

N,N- dimethylformamide

≤880ppm

Not detected

Triethylamine

≤320ppm

Not detected

Related compounds

Impurity a

≤0.10%

Not detected

Salicylic Acid

≤0.10%

Not detected

Salicylamine

≤0.05%

Not detected

Any other single impurity

≤0.05%

0.01%

Total impurities

≤03%

0.04%

Microbial enumeration

Total aerobic microbial count

≤1000 cfu/g

<10 cfu/g

Total molds and yeasts

≤100 cfu/g

<10 cfu/g

Assay (on drying basis )

98.0%~102.0%

100.0%

Conclusion

The test results meets the specification according to the in-house standard

Package: 1kg/bag; 25kg/drum

Storage conditions: Keep in dark place, Inert atmosphere,2-8°C

 

Safety Information

Dangerous goods label: Xn

Hazard category code: 22-36/38-43

Safety instructions: 26-36

WGK Germany: 3

RTECS number: GQ7000000

Customs code: 2924296000

 

What is the application of Deferasirox API

1. Deferasirox API can be used to treat reversible renal insufficiency caused by Fanconi syndrome.

2. Used for the treatment of secondary hemochromatosis.

3. Can be used to treat delayed skin porphyria.

4. Used for the treatment of myelodysplastic syndrome.

5. Used to treat iron overload caused by blood transfusion in patients with chronic anemia aged 2 years and above.

 

Preparation method

Salicylic acid is used as the raw material, and salicylic acid chloride is chlorinated with sulfoxide chloride to obtain salicylic acid chloride. Salicylic acid chloride and salicylic acid amide are obtained under high-temperature and vacuum distillation conditions instead of ordinary reflux method to obtain intermediates. Through high-temperature and vacuum distillation, a large amount of low boiling substances and by-products can be evaporated, increasing the mass fraction of the intermediates from 88.7% to 97.5%. Finally, the carboxylphenyl hydrazine hydrochloride was first removed from hydrochloric acid and cyclized with the intermediate to prepare the product of delaros, reducing the operations of desalination and solvent evaporation in post-reaction treatment, as well as reducing the amount of anhydrous ethanol used, making the operation more convenient.

1. Preparation of Salicylyl Chloride (Compound 1)

Add salicylic acid (13.8g, 0.1mol), 10 drops of anhydrous pyridine, and 10mL of sulfoxide chloride to the reaction flask, stir at room temperature for 30 minutes, slowly raise the temperature to 70 ℃, stir until almost no hydrogen chloride gas is released, then raise the temperature to 80 ℃, and stir for 3 hours. The remaining sulfoxide chloride is evaporated under reduced pressure to obtain a light yellow liquid, which is cooled to precipitate crystals and directly used for the next reaction.

Preparation of 2.2- (2-hydroxyphenyl) - [1,3] benzozinone (compound 2)

Add salicylamide (13.7g, 0.1mol) and compound 1 obtained from the previous reaction to the reaction bottle equipped with a distillation device, heat to 180 ℃, and perform vacuum distillation for 3 hours while reacting to remove the water obtained from the reaction. Add 50mL of anhydrous ethanol under melting (insulation), precipitate solid yellow product, filter, and recrystallize anhydrous ethanol to obtain 16.8g of yellow product with a yield of 70.3%, mp210-2 Chemicalbook 13 ℃.

3. Preparation of Carboxyphenylhydrazine Hydrochloride (Compound 3)

Add 6.85g, 0.05mol of para aminobenzoic acid and 10mL of distilled water to a 250mL three necked flask, stir until a paste is formed. Drip 12.5mL of concentrated hydrochloric acid below 5 ° C, cool to 5 ° C in an ice salt bath, and slowly add a saturated solution of sodium nitrite (3.5g, 0.05mol) dissolved in a small amount of water (8g) for diazotization reaction while stirring. Control the reaction temperature below 5 ° C. After dripping, continue stirring for 30 minutes. Then pour this diazonium salt solution into a solution of sodium sulfite (25.2g, 0.2mol) pre cooled to 5 ° C and dissolved in water (100mL). Stir at this temperature for 30 minutes. Heat up to 80 ℃, hold for 1.5 hours, the orange red solution turns slightly yellow, cool to room temperature, slowly add hydrochloric acid to acidify to pH 3, obtain the precipitation of p-carboxyphenylhydrazine hydrochloride, filter, air dry, and set aside to obtain 8.3g of white product with a yield of 88.3%.

4. Preparation of Dilaros

Adjust the pH value of compound 3 (3.8g, 0.02mol) to 6 with 30% NaOH, stir, let it stand for layering, and separate the water layer. The oil layer is p-carboxyphenylhydrazine. Place the oil layer in a flask, add compound 2 (5.0g, 0.02mol), and reflux in anhydrous ethanol solution (75mL) for 2 hours. Cool, precipitate crystals, filter, wash with 10mL ice ethanol, dry, and recrystallize with ethanol water to obtain 6.3g of slightly yellow product with a yield of 84.45%.

 

Our Advantage

Rich experience: we have 13 Years of professional experience;

Customers all over the world: sell to more than 100 countries;

Provide diversified products: the products have been applied to all major international brands in the fields of drugs, dietary supplements, cosmetics, animal nutrition and functional food.

Price advance: low MOQ with competitive price;

Quality certification: ISO; Halal; Kosher certified

After-sales service: Professional team 7*24 hours customer service.

 

In conclusion

In summary, Xi'an Yihui company as a professional Deferasirox API manufacturer has strong technical strength and advanced production equipment and is committed to providing customers with high-quality, efficient and reliable drug raw materials. if you need it, pls feel free to contact us any time. we will reply you asap.

our contact information:

E-mail: sales@yihuipharm.com
Tel: 0086-29-89695240
WeChat or WhatsApp: 0086-17792415937

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