Olmesartan Medoxomil
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Olmesartan Medoxomil 속성
- 녹는점
- 180°C
- 끓는 점
- 804.2±75.0 °C(Predicted)
- 밀도
- 1.38±0.1 g/cm3(Predicted)
- 인화점
- 180°C
- 저장 조건
- 2-8°C
- 용해도
- DMSO: 용해성20mg/mL, 투명
- 산도 계수 (pKa)
- 4.15±0.10(Predicted)
- 물리적 상태
- 가루
- 색상
- 흰색에서 베이지색
- 분해온도
- 180 ºC
- InChIKey
- UQGKUQLKSCSZGY-UHFFFAOYSA-N
- SMILES
- C1(CCC)N(CC2=CC=C(C3=CC=CC=C3C3=NNN=N3)C=C2)C(C(OCC2=C(C)OC(=O)O2)=O)=C(C(O)(C)C)N=1
- CAS 데이터베이스
- 144689-63-4(CAS DataBase Reference)
안전
- 위험 및 안전 성명
Olmesartan Medoxomil C화학적 특성, 용도, 생산
개요
Olmesartan medoxomil was launched in the US as benicar(R), 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.화학적 성질
White to off-white crystalline powder용도
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.
일반 설명
Olmesartan Medoxomil is a synthetic imidazole derivative prodrug with an antihypertensive property. Upon hydrolysis, olmesartan medoxomil is converted to olmesartan. Olmesartan selectively binds to the angiotensin type 1 (AT1) receptor of angiotensin II in vascular smooth muscle and adrenal gland, thereby competing angiotensin II binding to the receptor. This prevents angiotensin II-induced vasoconstriction and decreases aldosterone production, thereby preventing aldosterone-stimulated sodium retention and potassium excretion.부작용
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.Synthesis
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.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 준비 용품 및 원자재
원자재
Trityl olmesartan
Ethyl 4-(1-hydroxy-1-methylethyl)-2-propyl-imidazole-5-carboxylate
5-(4'-Bromomethyl-1,1'-biphenyl-2-yl)-1-triphenylmethyl-1H-tetrazole
N-Trityl Olmesartan Ethyl Ester
Trityl Olmesartan Medoxomil
1H-IMidazole-5-carboxylic acid, 4-(1-hydroxy-1-Methylethyl)-2-propyl-1-[[2'-[1-(triphenylMethyl)-1H-tetrazol-5-yl][1,1'-biphenyl]-4-yl]Methyl]-, ethyl ester
4-Cloromethyl-5-methyl-1,3-dioxol-2-one
준비 용품
Olmesartan Medoxomil 공급 업체
글로벌( 762)공급 업체
공급자 | 전화 | 이메일 | 국가 | 제품 수 | 이점 |
---|---|---|---|---|---|
Shandong Hengshannuode Pharmaceutical Technology Co., Ltd. | +8615065888978 |
admin@hsnordpharma.com | China | 92 | 58 |
Sinoway Industrial co., ltd. | 0592-5800732; +8613806035118 |
xie@china-sinoway.com | China | 992 | 58 |
Henan Tengmao Chemical Technology Co. LTD | +8615238638457 |
salesvip2@hntmhg.com | China | 415 | 58 |
Shandong Huisheng Import & Export Co., Ltd. | +86-13176845580 +86-13176845580 |
da@zhongda-biotech.com | China | 248 | 58 |
Anhui Zhongda Biotechnology Co., Ltd | +8619956560829 |
justine@zhongda-biotech.com | China | 300 | 58 |
Anhui Zhongda Biotechnology Co., Ltd | +8615689548120 |
linda@zhongda-biotech.com | China | 204 | 58 |
Anhui Ruihan Technology Co., Ltd | +8617756083858 |
daisy@anhuiruihan.com | China | 994 | 58 |
Beijing Cooperate Pharmaceutical Co.,Ltd | 010-60279497 |
sales01@cooperate-pharm.com | CHINA | 1811 | 55 |
Henan Tianfu Chemical Co.,Ltd. | +86-0371-55170693 +86-19937530512 |
info@tianfuchem.com | China | 21691 | 55 |
Jiangsu Zhongbang Pharmaceutical Co., Ltd. | 025-87151996 |
zbsales@chinaredsun.com | CHINA | 32 | 55 |
Olmesartan Medoxomil 관련 검색:
Olmesartan
Olmesartan
OlMesartan Lactone IMpurity
1-(4-(2-hydroxypropan-2-yl)-2-propyl-1-((2'-(1-trityl-1H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-1H-imidazol-5-yl)ethanone
Losartan potassium
Irbesartan
Olmesartan
Rebeprazole sodium
Valganciclovir hydrochloride
4-(1-Methoxy-1-methylethyl)-2-propyl-1H-Imidazole-5-carboxylic acid ethyl ester
Anastrozole
Tasosartan
EPROSARTAN
4,5-Bismethylene-1,3-dioxolan-2-one
Dehydro Olmesartan
OlMesartan MedoxoMil Ethyl Methyl Analog
Diethyl 2-propylImidazoledicarbonate
OlMesartan MedoxoMil Butyl IMpurity