ChemicalBook > CAS DataBase List > Azilsartan kaMedoxoMil

Azilsartan kaMedoxoMil

Product Name
Azilsartan kaMedoxoMil
CAS No.
863031-24-7
Chemical Name
Azilsartan kaMedoxoMil
Synonyms
TAK 491 kamedoxomil;TAK-491 monopotassium;Azilsartan kaMedoxoMil;Azilsartan KaModoxoMil;Azilsartan KaMedoximil;Azilsartan Mehtyl ester;Azilsartan MedoxMil PotassuiM;Azilsartan Medoxomil Potassium;Azilsartan MedoxiMil PotassiuM;Azilsartan MedoxoMil PotassiuM salt
CBNumber
CB92549391
Molecular Formula
C30H25KN4O8
Formula Weight
608.65
MOL File
863031-24-7.mol
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Azilsartan kaMedoxoMil Property

Melting point:
193 - 195°C
storage temp. 
Refrigerator, Under inert atmosphere
solubility 
DMSO (Slightly), Methanol (Slightly)
form 
Solid
color 
White to Off-White
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Hazard and Precautionary Statements (GHS)

Symbol(GHS)
Signal word
Warning
Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P301+P312IF SWALLOWED: call a POISON CENTER or doctor/physician IF you feel unwell.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

TRC
Product number
A965605
Product name
AzilsartanKamedoxomil(>90%)
Packaging
250mg
Price
$425
Updated
2021/12/16
Usbiological
Product number
260001
Product name
Azilsartan medoxomil potassium
Packaging
250mg
Price
$701
Updated
2021/12/16
Biorbyt Ltd
Product number
orb146200
Product name
Azilsartan kamedoxomil
Purity
>98%
Packaging
250mg
Price
$912.9
Updated
2021/12/16
ApexBio Technology
Product number
B1071
Product name
Azilsartanmedoxomilmonopotassium
Packaging
50mg
Price
$1347
Updated
2021/12/16
Biorbyt Ltd
Product number
orb146200
Product name
Azilsartan kamedoxomil
Purity
>98%
Packaging
1g
Price
$1802
Updated
2021/12/16
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Azilsartan kaMedoxoMil Chemical Properties,Usage,Production

Uses

Azilsartan Kamedoxomil is an angiotensin II receptor blocker.

Definition

ChEBI: An organic potassium salt that is the monopotassium salt of azilsartan medoxomil. A prodrug for azilsartan, it is used for treatment of hypertension.

Clinical Use

Azilsartan kamedoxomil, developed by Takeda Pharmaceuticals, was approved for the treatment of hypertension and launched in the U.S. under the brand name Edarbi. Edarbi is a prodrug that undergoes rapid hydrolysis to liberate azilsartan, the active ingredient (TAK-536, 39). As the 8th angiotensin receptor blocker (ARB) to enter the world market, azilsartan kamedoxomil can function as monotherapy or in combination with other antihypertensive agents. In several clinical studies, monotherapeutic azilsartan kamedoxomil showed superior antihypertensive activity and a favorable safety/tolerability profile in patients compared with other established therapeutics, including valsartan, olmesartan medoxomil, candesartan, and telmisartan.In late 2011,Takeda announced that FDA also approved the fixed-dose combination tablet of azilsartan kamedoxomil with chlorthalidone under the trade name of Edarbyclor.

Synthesis

Based on the synthesis of azilsartan, the process-scale approach to azilsartan kamedoxomil is described in the scheme. The synthesis started with commercially available methyl 2-[(tert-butoxycarbonyl)amino]-3-nitrobenzoate (30), which can also be prepared by several different routes.41,42 Alkylation of 30 with diaryl bromide 31 gave benzylamine 32 in 78% yield, which was followed by deprotection with 30% ethanolic HCl and alkalinization to produce amine 33 in 77% yield. The nitro group within 33 was reduced with hydrazine hydrate and a catalytic amount of ferric chloride to afford 2,3-diaminobenzoate 34 in 64% yield. Ring formation was achieved by treatment of 34 with tetraethoxymethane and acetic acid to produce benzimidazole 35 in 91% yield.37 The addition of hydroxylamine to the cyano group of 35 provided amidoxime 36 in 55% yield, which underwent immediate cyclization upon treatment with 2-ethylhexyl chloroformate 37 in refluxing xylenes to give oxadiazolone 38 in 52% yield. Hydrolysis of 38 gave azilsartan (39, TAK-536) in 94% yield. In the presence of perchlorobenzoyl chloride 40 and triethylamine, carboxylic acid 39 was converted to the mixed acid anhydride intermediate, which when condensed with alcohol 41 furnished benzoate 42 in 50% yield. Salt preparation of 42 was accomplished with potassium 2-ethylhexyl carboxylate 43 affording azilsartan kamedoxomil (V) in 63% yield.

Azilsartan kaMedoxoMil Preparation Products And Raw materials

Raw materials

Preparation Products

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Azilsartan kaMedoxoMil Suppliers

Shandong Luning Pharmaceutical Co., Ltd.
Tel
13371546309
Country
China
ProdList
10
Advantage
58
Hubei Chenxin Pharmaceutical Co., Ltd.
Tel
18696113233
Fax
QQ:2544920688
Email
like1076463918@163.com
Country
China
ProdList
3055
Advantage
58
Nanjing Chemlin Chemical Co., Ltd
Tel
025-83697070
Fax
+86-25-83453306
Email
info@chemlin.com.cn
Country
China
ProdList
18089
Advantage
64
Chengdu Yuyang High-Tech Developing Co., Ltd
Tel
+86-28-61777709
Fax
+86-28-61777709
Email
yygk@yygk.com
Country
China
ProdList
69
Advantage
58
Haoyuan Chemexpress Co., Ltd.
Tel
021-58950125
Fax
(86) 21-58955996
Email
info@chemexpress.com
Country
China
ProdList
7553
Advantage
61
MedChemexpress LLC
Tel
021-58955995
Fax
609-228-5909
Email
sales@medchemexpress.cn
Country
United States
ProdList
4863
Advantage
58
Nanjing Sunlida Biological Technology Co., Ltd.
Tel
025-57798810
Fax
025-57019371
Email
sales@sunlidabio.com
Country
China
ProdList
3750
Advantage
55
Hubei lansan Biochemical Pharmaceutical Co., Ltd.
Tel
86-714-6395877
Fax
86-714-6395835
Country
China
ProdList
26
Advantage
58
Zhengzhou Topcare Pharmaceutical Co.,Ltd.
Tel
0371-60942985
Fax
0371-60942986,qq1994339443
Country
China
ProdList
54
Advantage
58
Shanghai YuLue Chemical Co., Ltd.
Tel
021-60345187 13671753212
Fax
021-34702061
Email
lzz841106@aliyun.com
Country
China
ProdList
10287
Advantage
55
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View Lastest Price from Azilsartan kaMedoxoMil manufacturers

Career Henan Chemical Co
Product
Azilsartan kaMedoxoMil 863031-24-7
Price
US $1.00/kg
Min. Order
1kg
Purity
98%
Supply Ability
1000KG
Release date
2018-12-16

863031-24-7, Azilsartan kaMedoxoMilRelated Search:


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  • 863031-24-7
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  • 863031-24-7