Carvedilol CAS 72956-09-3 Purity >99.0% (HPLC)

Short Description:

Chemical Name: Carvedilol

CAS: 72956-09-3

Purity: >99.0% (HPLC)

Appearance: White Crystalline Powder

Contact: Dr. Alvin Huang

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72956-09-3 - Description:

Shanghai Ruifu Chemical Co., Ltd. is the leading manufacturer of Carvedilol (CAS: 72956-09-3) with high quality. Ruifu Chemical can provide worldwide delivery, competitive price, excellent service, small and bulk quantities available. Purchase Carvedilol, Please contact: alvin@ruifuchem.com

72956-09-3 - Intermediates of Carvedilol:

N-(2-(2-Methoxyphenoxy)ethyl)benzylamine Hydrochloride	CAS: 3246-03-5
2-(2-Methoxyphenoxy)ethylamine Hydrochloride Hydrate	CAS 64464-07-9
2-(2-Methoxyphenoxy)ethylamine	CAS 1836-62-0
4-(2,3-Epoxypropoxy)carbazole	CAS 51997-51-4
4-Hydroxycarbazole	CAS 52602-39-8
1,3-Cyclohexanedione	CAS 504-02-9
Carvedilol	CAS 72956-09-3
Carvedilol Phosphate Hemihydrate	CAS 610309-89-2

72956-09-3 - Chemical Properties:

Chemical Name	Carvedilol
Synonyms	1-(9H-Carbazol-4-yloxy)-3-[[2-(2-Methoxyphenoxy)ethyl]amino]-2-Propanol; Artist; Cadilan; Carca; Cardivas; Carloc; Carvas; Carvedilol; Carvediol; Coreg; DQ 2466; Dilatrend; Dimitone; Eucardic; Korvasan; Kredex; Querto; Talliton; BM-14190
Stock Status	In Stock, GMP Commercial
CAS Number	72956-09-3
Molecular Formula	C24H26N2O4
Molecular Weight	406.48 g/mol
Melting Point	115.0 to 119.0℃
Density	1.250±0.06 g/cm3
Solubility in Water	Insoluble in Water
Solubility	Soluble in Methanol. Slightly Soluble in Ethanol, Ether
Storage Temp.	Cool & Dry Place (2~8℃)
COA & MSDS	Available
Brand	Ruifu Chemical

72956-09-3 - Specifications:

Items	Inspection Standards	Results
Appearance	White Crystalline Powder	Complies
Loss on Drying	≤0.50% (105℃ for 3 h)	0.25%
Residue on Ignition	≤0.10%	0.07%
Related Substances
Total Impurities	≤0.50%	Complies
Impurity A	≤0.20%	Complies
Impurity C	≤0.02%	Complies
Any Other Individual Impurity	≤0.10%	Complies
Heavy Metals (Pb)	≤10ppm	<10ppm
Purity / Analysis Method	>99.0% (HPLC)	99.72%
Infrared Spectrum	Conforms to Structure	Complies
Conclusion	The product has been tested & complies with the specifications

72956-09-3 - Package/Storage/Shipping:

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

72956-09-3 - 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

72956-09-3 - 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 Assurance? Strict 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.

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

Factory Audit? Factory audit welcome. Please make an appointment in advance.

MOQ? No MOQ. Small order is acceptable.

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

Transportation? By Express (FedEx, DHL), by Air, by Sea.

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

Custom Synthesis? Can provide custom synthesis services to best fit your research needs.

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

72956-09-3 - Safety Information:

Hazard Codes N,Xn
Risk Statements 51/53-36/37/38-20/21/22
Safety Statements 61-36-26
RIDADR UN 3077 9/PG 3
WGK Germany 3
RTECS UA8670000
HazardClass IRRITANT
PackingGroup III
Hazardous Substances Data 72956-09-3(Hazardous Substances Data)
Toxicity LD50 oral in dog: > 1gm/kg

72956-09-3 - Application:

Carvedilol (CAS: 72956-09-3) is a vasodilating beta-blocker useful in the treatment of hypertension and angina pectoris. In addition to lowering blood pressure, carvedilol decreases total vascular resistance without the reflex tachycardia usually occurring with vasodilators. It is reported to be well tolerated with renal sparing effects.

Carvedilol was first launched in Belgium in 1985. This product can block alpha and beta receptors, no intrinsic activity, in high concentrations of fashion with calcium antagonism. It has a strong effect of blocking beta receptors, which can expand blood vessels, reduce peripheral resistance and lower blood pressure, and has little effect on cardiac output and heart rate. Clinical can be used for primary hypertension and angina pectoris.

72956-09-3 - USP 35 Standard:

DEFINITION

Carvedilol contains NLT 98.0% and NMT 102.0% of C24H26N2O4, calculated on the dried basis.

IDENTIFICATION

• A. Infrared Absorption <197K>

• B. The retention time of the major peak of the Sample solution corresponds to that of the Standard solution, as obtained in the Assay.

ASSAY

• Procedure

Buffer: 2.72 g/L of monobasic potassium phosphate. Adjust with dilute phosphoric acid to a pH of 2.0.

Mobile phase: Acetonitrile and Buffer (31:69)

System suitability solution: 0.05 mg/mL each of USP Carvedilol RS and USP Carvedilol Related Compound A RS in Mobile phase

Standard solution: 0.04 mg/mL of USP Carvedilol RS in Mobile phase

Sample solution: 0.04 mg/mL of Carvedilol in Mobile phase

Chromatographic system

(See Chromatography <621>, System Suitability.)

Mode: LC

Detector: UV 240 nm

Column: 4.6-mm × 15-cm; 5-µm packing L7

Column temperature: 55℃

Flow rate: 1 mL/min

Run time: 60 min

Injection size: 10 µL

System suitability

Sample: System suitability solution

Suitability requirements

Resolution: NLT 4.0 between carvedilol and carvedilol related compound A

Tailing factor: NMT 1.5 for the carvedilol peak

Relative standard deviation: NMT 2%

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of carvedilol (C24H26N2O4) in the portion of the sample taken:

Result = (rU/rS) × (CS/CU) × 100

rU=	peak response of carvedilol from the Sample solution
rS=	peak response of carvedilol from the Standard solution
CS=	concentration of carvedilol in the Standard solution (mg/mL)
CU=	concentration of Carvedilol in the Sample solution (mg/mL)

Acceptance criteria: 98.0%-102.0% on the dried basis

IMPURITIES

• Residue on Ignition <281>: NMT 0.1% from 1 g

• Heavy Metals, Method II <231>: NMT 10 ppm

• Organic Impurities, Procedure 1: [Note-On the basis of the impurities present, perform either Organic Impurities, Procedure 1 or Organic Impurities, Procedure 2. Organic Impurities, Procedure 2 is recommended when carvedilol related compound F is a potential impurity.]

Buffer and Mobile phase: Prepare as directed in the Assay.

System suitability solution: 0.05 mg/mL each of USP Carvedilol RS and USP Carvedilol Related Compound C RS in Mobile phase

Standard solution: 1 µg/mL each of USP Carvedilol RS, USP Carvedilol Related Compound A RS, USP Carvedilol Related Compound B RS, USP Carvedilol Related Compound D RS, and USP Carvedilol Related Compound E RS, and 0.2 µg/mL of USP Carvedilol Related Compound C RS in Mobile phase

Sample solution: 1 mg/mL of Carvedilol in Mobile phase

Chromatographic system

(See Chromatography <621>, System Suitability.)

Mode: LC

Detector: Dual wavelength, UV 220 and 240 nm. Use 220 nm for quantitating carvedilol related compound E, and use 240 nm for carvedilol and all other related compounds.

Column: 4.6-mm × 15-cm; 5-µm packing L7

Column temperature: 55℃

Flow rate: 1 mL/min

Injection size: 20 µL

System suitability

Sample: System suitability solution

Suitability requirements

Resolution: NLT 17 between carvedilol and carvedilol related compound C

Analysis

Samples: Standard solution and Sample solution

Calculate the percentage of carvedilol related compound A, carvedilol related compound B, carvedilol related compound C, carvedilol related compound D, carvedilol related compound E, and any other individual impurity in the portion of Carvedilol taken:

Result = (rU/rS) × (CS/CU) × 100

rU	=	peak response of the corresponding related compound or any other impurity from the Sample solution
rS	=	peak response of the corresponding related compound from the Standard solution. To calculate the percentage of any other individual impurity use the peak response of carvedilol.
CS	=	concentration of the corresponding related compound in the Standard solution (mg/mL). To calculate the percentage of any other impurities for CS, use the concentration of USP Carvedilol RS.
CU	=	concentration of Carvedilol in the Sample solution (mg/mL)

Acceptance criteria: See Table 1.

Table 1

Name	Relative Retention Time	Acceptance Criteria, NMT (%)
Carvedilol related compound Ea	0.35	0.1
Carvedilol related compound Ab	0.52	0.1
Carvedilol bisalkylpyrocatechol derivative (if present)c	0.70	0.15
Carvedilol	1.0	—
Carvedilol related compound Cd	3.6	0.02
Carvedilol related compound De	5.0	0.1
Carvedilol related compound Bf	8.5	0.1
Any other individual impurity	-	0.10
Total impurities	-	0.5g
a 2-(2-Methoxyphenoxy)ethyl amine. b 1-(4-(2-Hydroxy-3-(2-(2-methoxyphenoxy)ethylamino)propoxy)-9H-carbazol-9-yl)-3-(2-(2-methoxyphenoxy)ethylamino) propan-2-ol. c 3,3¢-{2,2¢-[1,2-Phenylenebis(oxy)]bis(ethane-2,1-diyl)}bis(azanediyl)bis(1-(9H-carbazol-4-yloxy)propan-2-ol). d 1-(9H-Carbazol-4-yloxy)-3-(benzyl(2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol. e 4-(Oxiran-2-ylmethoxy)-9H-carbazole. f 3,3¢-(2-(2-Methoxyphenoxy)ethylazanediyl)bis(1-(9H-carbazol-4-yloxy)propan-2-ol). g Disregard any impurity less than 0.01%.

• Organic Impurities, Procedure 2

Solution A: Acetonitrile and trifluoroacetic acid (100:0.1)

Solution B: Trifluoroacetic acid and water (0.1:100)

Diluent: Acetonitrile, trifluoroacetic acid, and water (22:0.1:78)

Mobile phase: See Table 2

Table 2

Time (min)	Solution A (%)	Solution B (%)
0	22	78
20	22	78
33	38	62
45	38	62
55	55	45
65	55	45
68	22	78
80	22	78

System suitability solution: 1.0 mg/mL of USP Carvedilol System Suitability Mixture RS in Diluent

Sample solution: 1 mg/mL of Carvedilol in Diluent

Chromatographic system

(See Chromatography <621>, System Suitability.)

Mode: LC

Detector: UV 240 nm

Column: 4.6-mm x 15-cm; 5-µm packing L68

Column temperature: 30℃

Flow rate: 1.4 mL/min

Injection size: 20 µL

System suitability

Sample: System suitability solution

Suitability requirements

Resolution: NLT 1.8 between carvedilol and carvedilol related compound F

Analysis

Sample: Sample solution

Calculate the percentage of each impurity in the portion of Carvedilol taken:

Result = (rU/rT) × 100

rU	=	peak response for each impurity in the Sample solution
rT	=	sum of all the peak responses in the Sample solution

Acceptance criteria: See Table 3.

Table 3

Name	Relative Retention Time	Acceptance Criteria, NMT (%)
Carvedilol related compound Aa	0.7	0.1
Carvedilol	1.0	—
Carvedilol related compound Fb	1.2	0.1c
N-Isopropylcarvedilold	1.6	0.1
Carvedilol related compound Ce	1.8	0.02
Carvedilol related compound Bf	2.1	0.1
Biscarbazoleg	3	0.1
Any other individual impurity	—	0.1
Total impurities	—	0.5
a 1-(4-(2-Hydroxy-3-(2-(2-methoxyphenoxy)ethylamino)propoxy)-9Hcarbazol-9-yl)-3-(2-(2-methoxyphenoxy)ethylamino) propan-2-ol. b 1-(2-(2-Methoxyphenoxy)ethylamino)-3-(6,7,8,9-tetrahydro-5H-carbazol-4-yloxy)propan-2-ol. c This impurity is quantitated using the procedure under Organic Impurities, Procedure 3: Carvedilol Related Compound F. d 1-(H-Carbazol-4-yloxy)-3-[[2-(2-methoxyphenoxy)ethyl]N-isopropylamino]-2-propanol. e 1-(9H-Carbazol-4-yloxy)-3-(benzyl(2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol. f 3,3'-(2-(2-Methoxyphenoxy)ethylazanediyl)bis(1-(9H-carbazol-4-yloxy)propan-2-ol). g 1,3-Bis-(9H-carbazol-4-yloxy)-2-propanol.

• Organic Impurities, Procedure 3: Carvedilol Related Compound F (if present)

Solution A: Trifluoroacetic acid and water (0.5:100)

Solution B: Methanol and trifluoroacetic acid (100:0.5)

Diluent: Water and acetonitrile (1:1)

Mobile phase: Solution A and Solution B (65:35)

System suitability solution: 1.5 mg/mL of USP Carvedilol System Suitability Mixture RS in Diluent

Sample solution: 1.5 mg/mL of Carvedilol in Diluent prepared as follows. Use about 1.9 mL of Diluent per mg of the Carvedilol, and sonicate briefly to facilitate dissolution.

Chromatographic system

(See Chromatography <621>, System Suitability.)

Mode: LC

Detector: UV 226 nm

Column: 4.6-mm × 30-mm; 3-µm packing L7

Column temperature: 40℃

Flow rate: 2 mL/min

Injection size: 10 µL

System suitability

Sample: System suitability solution

Suitability requirements

Resolution: NLT 2.0 between carvedilol and carvedilol related compound F

Analysis

Sample: Sample solution

Calculate the percentage of carvedilol related compound F in the portion of the sample taken:

Result = (rU/rT) × (1/F) × 100

rU	=	peak response of carvedilol related compound F from the Sample solution
rT	=	sum of the peak responses of carvedilol and carvedilol related compound F from the Sample solution
F	=	relative response factor, 1.1

Acceptance criteria: NMT 0.1%

SPECIFIC TESTS

• Loss on Drying <731>: Dry a sample at 105℃ for 3 h: it loses NMT 0.5% of its weight.

ADDITIONAL REQUIREMENTS

• Packaging and Storage: Preserve in tight containers, and store at controlled room temperature.

• Labeling: If a test for Organic Impurities by HPLC other than Procedure 1 is used, then the labeling states the test with which the article complies.

• USP Reference Standards <11>

USP Carvedilol RS

USP Carvedilol Related Compound A RS
1-(4-(2-Hydroxy-3-(2-(2-methoxyphenoxy)ethylamino)propoxy)-9H-carbazol-9-yl)-3-(2-(2-methoxyphenoxy)ethylamino) propan-2-ol.
C36H43N3O7 629.74

USP Carvedilol Related Compound B RS
3,3'-(2-(2-Methoxyphenoxy)ethylazanediyl)bis(1-(9H-carbazol-4-yloxy)propan-2-ol).
C39H39N3O6 645.74

USP Carvedilol Related Compound C RS
1-(9H-Carbazol-4-yloxy)-3-(benzyl(2-(2-methoxyphenoxy)ethyl)amino)propan-2-ol.
C31H32N2O4 496.60

USP Carvedilol Related Compound D RS
4-(Oxiran-2-ylmethoxy)-9H-carbazole.
C15H13NO2 239.27

USP Carvedilol Related Compound E RS
2-(2-Methoxyphenoxy)ethyl amine.
C9H13NO2 167.21

USP Carvedilol System Suitability Mixture RS
Mixture of approximately 0.1% carvedilol related compound F (1-(2-(2-Methoxyphenoxy)ethylamino)-3-(2,3,4,9-tetrahydro-1H-carbazol-5-yloxy)propan-2-ol) in a matrix of carvedilol drug substance.