Vardenafil Intermediate CAS 224789-21-3 Purity >99.0% (HPLC)

Short Description:

Chemical Name: 2-(2-Ethoxyphenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]triazin-4(3H)-one 

CAS: 224789-21-3

Purity: >99.0% (HPLC)

Appearance: Off-White to Pale Yellow Powder

Intermediate of Vardenafil / Vardenafil Hydrochloride

Contact: Dr. Alvin Huang

Mobile/Wechat/WhatsApp: +86-15026746401

E-Mail: alvin@ruifuchem.com


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224789-21-3 - Description:

Shanghai Ruifu Chemical Co., Ltd. is the leading manufacturer of 2-(2-Ethoxyphenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]triazin-4(3H)-one (CAS: 224789-21-3) with high quality, intermediate of Vardenafil. Ruifu Chemical can provide worldwide delivery, competitive price, excellent service, small and bulk quantities available. Purchase Vardenafil Intermediates, Please contact: alvin@ruifuchem.com

224789-21-3 - Chemical Properties:

Chemical Name 2-(2-Ethoxyphenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]triazin-4(3H)-one
Synonyms Vardenafil Dessulfonyl Impurity; 2-(2-Ethoxyphenyl)-5-Methyl-7-Propyl-3H-Imidazo[5,1-F][1,2,4]triazin-4-one; Vardenafil Propyl Imidazotriazinone Impurity; Vardenafil Related Compound 1
Stock Status In Stock, Production Capacity 2 Tons per Month   
CAS Number 224789-21-3
Molecular Formula C17H20N4O2
Molecular Weight 312.37 g/mol
Melting Point 142.0~148.0℃ 
Density 1.26±0.10 g/cm3 
Long-Term Storage  Cool & Dry Place (2~8℃) 
COA & MSDS Available
Origin Shanghai, China
Brand Ruifu Chemical

224789-21-3 - Specifications:

Items Specifications  Results
Appearance Off-White to Pale Yellow Powder Off-White Powder  
Melting Point 142.0~148.0℃ 146.0~147.0℃
Loss on Drying <1.00% (102℃, 3h) 0.23% 
Heavy Metals (Pb) ≤20ppm <20ppm 
Purity / Analysis Method >99.0% (HPLC)  99.79% 
1H NMR Spectrum Consistent with Structure Complies
Conclusion The product has been tested and complies with the given specifications
Application Intermediate of Vardenafil / Vardenafil Hydrochloride 

Package/Storage/Shipping:

Package: Bottle, Aluminium foil bag, 25kg/Cardboard Drum, or according to customer's requirement.
Storage Condition: Keep the container tightly closed and store in a cool, dry (2~8℃) and well-ventilated warehouse away from incompatible substances. Protect from sunlight and moisture.
Shipping: Deliver to worldwide by air, by FedEx / DHL Express. Provide fast and reliable delivery. 

224789-21-3 - ROS:

www.ruifuchemical.com

224789-21-3 - Analysis Method:

1. Appearance: Put the sample on white paper and observe the appearance, off-white to pale yellow powder.
2. Analysis:
2.1 Melting Point determination according to law (Chinese Pharmacopoeia 2010 Edition II Appendix ⅥC) Melting point is 142.0~148.0℃.
2.2 Loss on Drying: Determination according to law (Appendix ⅧL, Part II, 2010 Edition of Chinese Pharmacopoeia). Precision weighing appropriate amount of this product, dry at 102℃ for 3 hours, weight loss shall not be more than 1.00%.
2.3 Heavy Metals: Determination according to law (People's Republic of China Pharmacopoeia 2010 Edition, Part II Appendix ⅧH) Determination by the second method.
Precision weigh 1.0g of the test product, slowly burning until completely carbonized, cool, add 0.5-1.0ml sulfuric acid, make it moist, heat at low temperature until the sulfuric acid is exhausted, add 0.5ml nitric acid, steam dry, until the nitrogen oxide vapor is exhausted, cool, hot at 500-600℃ to completely carbonized, cool, add 2ml hydrochloric acid, After drying in a water bath, add 15ml water, drop the ammonia test solution until it becomes neutral to the phenolphthalein indicator solution, add 2ml acetate buffer (ph3.5), and slightly heat dissolve, move it to the Nachner colorimetric tube, and dilute it into 25ml with water. Take another reagent for preparing the test solution, and steam it in a porcelain dish, add 2ml acetate buffer (PH3.5) and 15ml water to slightly heat After dissolution, move the Nath colorimetric tube, add a certain amount of standard lead solution, and then dilute with water to 25ml. Colorimetric experiment is carried out between test solution and standard solution to obtain. Standard solution preparation according to (People's Republic of China Pharmacopoeia 2010 edition II Appendix Ⅷ Heavy metal test method) the first method. Heavy metals must not exceed 20 parts per million.
3. Purity: According to high performance liquid chromatography, determined according to law (Chinese Pharmacopoeia 2010 edition II Appendix VD).
Chromatographic conditions:
Column: C18, 200mm×4.6mm, 5μm;
Mobile phase: Phosphate buffer (weigh 2.72g potassium dihydrogen phosphate, add water to dissolve and dilute to 1000ml, adjust pH=3.5) : acetonitrile: = 35:65;
Detection wavelength: 254nm;
Flow rate: 1.0ml/min.
Determination method: Take about 30mg of this product, weigh it accurately, dilute it with mobile phase to make the concentration of about 0.3mg/ml, take 20μl into the liquid chromatograph, record the chromatogram. According to area normalization method, the purity is not less than 99.0%. 

Advantages:

Sufficient Capacity: Sufficient facilities and technicians

Professional Service: One stop purchasing service

OEM Package: Custom package and label available

Fast Delivery: If within stock, three days delivery guaranteed

Stable Supply: Maintain reasonable stock    

Technical Support: Technology solution available

Custom Synthesis Service: Ranged from grams to kilos

High Quality: Established a complete quality assurance system

FAQ:

How to Purchase? Please contact Dr. Alvin Huang: sales@ruifuchem.com or alvin@ruifuchem.com 

15 Years Experience? We have more than 15 years of experience in the manufacture and export of a wide range of high quality pharmaceutical intermediates or fine chemicals.

Main Markets? Sell to domestic market, North America, Europe, India, Korea, Japanese, Australia, etc.

Advantages? Superior quality, affordable price, professional services and technical support, fast delivery.

Quality AssuranceStrict quality control system. Professional equipment for analysis include NMR, LC-MS, GC, HPLC, ICP-MS, UV, IR, OR, K.F, ROI, LOD, MP, Clarity, Solubility, Microbial limit test, etc.

SamplesMost products provide free samples for quality evaluation, shipping cost should be paid by customers.

Factory AuditFactory audit welcome. Please make an appointment in advance.

MOQ? No MOQ. Small order is acceptable.

Delivery Time? If within stock, three days delivery guaranteed.

TransportationBy Express (FedEx, DHL), by Air, by Sea.

Documents? After sales service: COA, MOA, ROS, MSDS, etc. can be provided.

Custom SynthesisCan provide custom synthesis services to best fit your research needs.

Payment TermsProforma invoice will be sent first after confirmation of order, enclosed our bank information. Payment by T/T (Telex Transfer), PayPal, Western Union, etc. 

224789-21-3 - Application:

2-(2-Ethoxyphenyl)-5-Methyl-7-Propylimidazo[5,1-F][1,2,4]triazin-4(3H)-one (CAS: 224789-21-3) is an intermediate of Vardenafil (CAS: 224785-90-4) / Vardenafil Hydrochloride (CAS: 224785-91-5). Vardenafil is a new PDE5 inhibitor launched for oral treatment of male erectile dysfunction and it has significant structural similarity with sildenafil (Viagra), which was the first PDE5 inhibitor introduced in 1998 for this indication.
Vardenafil was the second agent to be marketed and had the advantage that its onset time was not reduced by taking the medication on a full stomach . It is 30 times more potent as an inhibitor of PDE5 (mean IC50, 3.9 nM) than sildenafil and 10 times more potent than tadalafil, with a greater selectivity (>1,000 times) for human PDE5 than for human PDE2, PDE3, and PDE4 and moderate selectivity (>80 times) for PDE1. The PDE inhibitory selectivity and both the in vitro and in vivo potency of the new PDE5 inhibitor vardenafil. Vardenafil specifically inhibited the hydrolysis of cGMP by PDE5, with an IC50 of 0.7 nM (sildenafil 6.6 nM). The IC50 of vardenafil for PDE1 was 180 nM, for PDE6 11 nM, and for PDE2, PDE3 and PDE4 more than 1,000 nM.  

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