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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
Molecular Weight:
608.65
MDL Number:
MFCD24849277
MOL File:
863031-24-7.mol
MSDS File:
SDS
Last updated:2023-05-18 11:31:11

Azilsartan kaMedoxoMil Properties

Melting point 193 - 195°C
storage temp. Refrigerator, Under inert atmosphere
solubility DMSO (Slightly), Methanol (Slightly)
form Solid
color White to Off-White
FDA UNII WEC6I2K1FC

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H302-H315-H319-H335
Precautionary statements  P261-P280-P301+P312-P302+P352-P305+P351+P338

Azilsartan kaMedoxoMil price

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
TRC A965605 AzilsartanKamedoxomil(>90%) 863031-24-7 250mg $425 2021-12-16 Buy
Usbiological 260001 Azilsartan medoxomil potassium 863031-24-7 250mg $701 2021-12-16 Buy
Biorbyt Ltd orb146200 Azilsartan kamedoxomil >98% 863031-24-7 250mg $912.9 2021-12-16 Buy
ApexBio Technology B1071 Azilsartanmedoxomilmonopotassium 863031-24-7 50mg $1347 2021-12-16 Buy
Biorbyt Ltd orb146200 Azilsartan kamedoxomil >98% 863031-24-7 1g $1802 2021-12-16 Buy
Product number Packaging Price Buy
A965605 250mg $425 Buy
260001 250mg $701 Buy
orb146200 250mg $912.9 Buy
B1071 50mg $1347 Buy
orb146200 1g $1802 Buy

Azilsartan kaMedoxoMil Chemical Properties,Uses,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.

Synthesis_863031-24-7

Azilsartan kaMedoxoMil Preparation Products And Raw materials

Raw materials

Preparation Products

Global( 164)Suppliers
Supplier Tel Email Country ProdList Advantage
Henan Tianfu Chemical Co.,Ltd.
+86-0371-55170693 +86-19937530512 info@tianfuchem.com China 21691 55
career henan chemical co
+86-0371-86658258 sales@coreychem.com China 29914 58
Shenzhen Nexconn Pharmatechs Ltd
+86-755-89396905 +86-15013857715 admin@nexconn.com China 10248 58
HubeiwidelychemicaltechnologyCo.,Ltd
18627774460 faith@widelychemical.com CHINA 742 58
Chongqing Chemdad Co., Ltd
+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Fuxin Pharmaceutical
+86-021-021-50872116 +8613122107989 contact@fuxinpharm.com China 10297 58
Zhengzhou Alfa Chemical Co.,Ltd
+8618530059196 sale04@alfachem.cn China 12468 58
SIMAGCHEM CORP
+86-13806087780 sale@simagchem.com China 17367 58
AFINE CHEMICALS LIMITED
0571-85134551 info@afinechem.com CHINA 15377 58
Dayang Chem (Hangzhou) Co.,Ltd.
571-88938639 +8617705817739 info@dycnchem.com CHINA 52867 58

View Lastest Price from Azilsartan kaMedoxoMil manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
azilsartan kamedoxomil pictures 2022-09-15 azilsartan kamedoxomil
863031-24-7
US $40.00 / kg 1kg 99% Ex 20 tons Hebei Anda Technology Co., LTD
Azilsartan kaMedoxoMil pictures 2019-07-06 Azilsartan kaMedoxoMil
863031-24-7
US $1.00 / kg 1kg 98% 1000KG Career Henan Chemical Co
Azilsartan kaMedoxoMil 1-[[2'-(2,5-Dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylic acid (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester potassium salt Azilsartan MedoxoMil PotassiuM salt Azilsartan MedoxoMil (MonopotassiuM salt) Azilsartan MedoxoMil (MonopotassiuM) Azilsartan MedoxiMil PotassiuM Azilsartan KaModoxoMil Azilsartan kaMedoxoMil (with 5 ints.) Azilsartan MedoxMil PotassuiM 1H-BenziMidazole-7-carboxylic acid, 1-[[2'-(2,5-dihydro-5-oxo-1,2,4-oxadiazol-3-yl)[1,1'-biphenyl]-4-yl]Methyl] -2-ethoxy-, (5-Methyl-2-oxo-1,3-dioxol-4-yl)Methyl ester, potassiuM salt Azilsartan Medoxomil Potassium Azilsartan Mehtyl ester Azilsartan Impurity 50 Potassium Salt Azilsartan medoxomil monopotassium (TAK 491) Azilsartan KaMedoximil Azilsartan Medoxomil Potassium Crude Azilsartan Impurity 45 Potassium Salt (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 2-ethoxy-1-((2'-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-benzo[d]imidazole-7-carboxylate, potassium salt TAK 491 kamedoxomil TAK-491 monopotassium Azilsartan Impurity 60 Potassium Salt 863031-24-7 C30H23KN4O8 C30H23N4O8K Azilsartan Kamedoxomil 863031-24-7