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Olmesartan Medoxomil

synthesize metabolism Side effects
Olmesartan Medoxomil
Olmesartan Medoxomil structure
CAS No.
144689-63-4
Chemical Name:
Olmesartan Medoxomil
Synonyms
OMST;CS-866;Benicar;Olmetec;Oimesartan;Olmesartan Medoxomi;Olmesartan MedoxomiI;OlmesartanC29H30N6O6;Olmesartan medoxomil;OLMESARTAN MEDOXIMIL
CBNumber:
CB8254825
Molecular Formula:
C29H30N6O6
Formula Weight:
558.59
MOL File:
144689-63-4.mol

Olmesartan Medoxomil Properties

Melting point:
180°C
Boiling point:
804.2±75.0 °C(Predicted)
Density 
1.38±0.1 g/cm3(Predicted)
Flash point:
180°C
storage temp. 
2-8°C
solubility 
DMSO: soluble20mg/mL, clear
pka
4.15±0.10(Predicted)
form 
powder
color 
white to beige
Decomposition 
180 ºC
InChIKey
UQGKUQLKSCSZGY-UHFFFAOYSA-N
CAS DataBase Reference
144689-63-4(CAS DataBase Reference)
FDA UNII
6M97XTV3HD
SAFETY
  • Risk and Safety Statements
RTECS  NI4014200
HS Code  2934990002

Olmesartan Medoxomil price More Price(13)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Sigma-Aldrich Y0001424 Olmesartan medoxomil for system suitability European Pharmacopoeia (EP) Reference Standard 144689-63-4 $190 2021-03-22 Buy
Sigma-Aldrich Y0001405 Olmesartan medoxomil European Pharmacopoeia (EP) Reference Standard 144689-63-4 $190 2021-03-22 Buy
Sigma-Aldrich PHR1851 Olmesartan medoxomil Pharmaceutical Secondary Standard; Certified Reference Material 144689-63-4 200mg $192 2021-03-22 Buy
Sigma-Aldrich 1478367 Olmesartan medoxomil United States Pharmacopeia (USP) Reference Standard 144689-63-4 100mg $769 2021-03-22 Buy
TCI Chemical O0510 Olmesartan Medoxomil >98.0%(HPLC)(T) 144689-63-4 5g $233 2021-03-22 Buy

Olmesartan Medoxomil Chemical Properties,Uses,Production

synthesize

Olmesartan Medoxomil can be synthesized in 8 steps from diaminomaleonitrile by successive reactions with trialkylorthopropanoate to access 2-propyl-imidazole-45dicarbonitrile, conversion of the two nitrile functions to the corresponding ethyl esters, followed by methylmagnesium bromide addition to give the corresponding 4-(1-hydroxyalkyl)imidazole derivative.

metabolism

Olmesartan medoxomil is rapidly and completely bioactivated by ester hydrolysis to its active metabolite, olmesartan, during absorption from the gastrointestinal tract. Olmesartan has an absolute bioavailability of approximatively 26%, a mean elimination half-life of 14 h in patients with hypertension and is not further metabolized. Olmesartan medoxomil is well tolerated, has a side-effect profile similar to that of placebo and unlike ACE inhibitors, the incidence of dry cough is rare.

Side effects

Dizziness or lightheadedness may occur as your body adjusts to the medication. If any of these effects persist or worsen, tell your doctor or pharmacist promptly. To reduce the risk of dizziness and lightheadedness, get up slowly when rising from a sitting or lying position.

Description

Olmesartan medoxomil was launched in the US as benicar@, an orally administered treatment for hypertension. Olmesartan, is a new selective and competitive nonpeptide angiotensin II type 1 receptor antagonist and potently inhibits the Ang.ll-induced pressor responses. The drug competitively inhibited binding of [125I1]-All to AT1 receptors in bovine adrenal cortical membranes, but had no effect on binding to AT2 receptors in bovine cerebellar membranes. In comparative clinical studies in patients with essential hypertension, olmesartan reduced sitting cuff diastolic blood pressure significantly more than losartan, valdesartan and ibesartan, while reductions in systolic blood pressure were similar for all treatments. Olmesartan medoxomil was also shown to reduce blood pressure significantly more effectively than losartan and the ACE inhibitor captopril and as effectively as the pbloker atenolol.

Chemical Properties

White to off-white crystalline powder

Originator

Sanky (Japan)

Uses

An angiotensin II receptor antagonist. Used as an anti-hypertensive

Uses

Olmesartan medoxomil is an angiotensin II receptor antagonist used to treat high blood pressure. Olmesartan works by blocking the binding of angiotensin II to the AT1 receptors in vascular muscle. By blocking the binding rather than the synthesis of angiotensin II, olmesartan inhibits the negative regulatory feedback on renin secretion.
Olmesartan medoxomil is a pro-drug that is de-esterified to the active metabolite, olmesartan. Olmesartan has a dual method of elimination, with about 60% eliminated by the liver and the remainder by the kidney. In situations of impaired renal or hepatic function, the alternative excretion pathway can compensate for the compromised one. Olmesartan is not metabolized by the cytochrome P450 enzyme system and therefore has a low potential for metabolic drug interactions, a feature that may be of importance when treating patients on multiple drug regimens, such as the elderly. Olmesartan is well tolerated and has an excellent safety profile that is comparable to that of placebo. In addition, olmesartan provides 24-h blood pressure control with a once-daily dosing. In head-to-head studies, olmesartan delivered superior blood pressure reduction when compared with other angiotensin-II receptor antagonists at their recommended doses.

brand name

Benicar

Chemical Synthesis

The imidazole ring of olmesartan (18) was constructed with diaminomaleonitrile 155 and trimethylorthobutyrate (156) in CH3CN then xylene to give 157 in 96% yield. Acid hydrolysis of 157 in 6N HCl gave the dicarboxylic acid intermediate. After esterification of the diacid in ethanol in the presence of HCl, diester 158 was treated with MeMgCl to give 4-(1-hydroxyalkyl) imidazole 159 in 95% yield. Alkylation of 159 with biphenyl bromide 160 in the presence of potassium tbutoxide afforded 161 in 80% yield. Ester 161 was then hydrolyzed to free carboxylic acid 162 under basic conditions, and 162 was treated with chloride 163 in the presence of K2CO3 to give ester 164 in 88% yield from 161.Lastly, the trityl group was removed with 25% aqueous acetic acid to give olmesartan (18) in 81% yield.

Olmesartan Medoxomil Preparation Products And Raw materials

Raw materials

Preparation Products


Olmesartan Medoxomil Suppliers

Global( 449)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
Jiangsu Zhongbang Pharmaceutical Co., Ltd.
025-87151996
025-87151996 zbsales@chinaredsun.com CHINA 32 55
Shanghai Payne Pharmaceutical Technology Co.Ltd
18678586262 021-58123769
info@paynepharm.com China 1355 58
Shenzhen Excellent Biotech Co., Ltd.
13480692018
ramyan@ex-biotech.com;sale@ex-biotech.com CHINA 955 58
Shandong Hengshannuode Pharmaceutical Technology Co., Ltd.
13583348585
admin@hsnordpharma.com CHINA 92 58
Beijing Cooperate Pharmaceutical Co.,Ltd
010-60279497
010-60279497 sales01@cooperate-pharm.com CHINA 1817 55
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 22607 55
Hangzhou FandaChem Co.,Ltd.
008615858145714
+86-571-56059825 fandachem@gmail.com CHINA 8882 55
Guangzhou PI PI Biotech Inc
+8618371201331
020-81716319 sales@pipitech.com;87478684@qq.com China 3245 55
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 26734 60
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29961 58

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View Lastest Price from Olmesartan Medoxomil manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2021-09-29 Olmesartan Medoxomil
144689-63-4
US $0.00 / KG 1KG 99.0%,USP/EP 500KG/month WUHAN FORTUNA CHEMICAL CO., LTD
2021-08-12 Olmesartan Medoxomil
144689-63-4
US $0.00 / Kg/Bag 2Kg/Bag 99% up, High Density 20 tons Sinoway Industrial co., ltd.
2021-08-10 Olmesartan Medoxomil USP/EP/BP
144689-63-4
US $1.10 / g 1g 99.9% 100 Tons min Dideu Industries Group Limited

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