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ロサルタンカリウム

ロサルタンカリウム 化学構造式
124750-99-8
CAS番号.
124750-99-8
化学名:
ロサルタンカリウム
别名:
2-ブチル-4-クロロ-5-(ヒドロキシメチル)-1-[(2'-(1H-テトラゾール-5-イル)-1,1'-ビフェニル-4-イル)メチル]-1H-イミダゾール·カリウム塩;アラドイス;ロサルタンカリウム;2-ブチル-4-クロロ-1-[[2'-(1H-テトラゾール-5-イル)-1,1'-ビフェニル-4-イル]メチル]-1H-イミダゾール-5-メタノール·カリウム;ニューロタン;2-ブチル-4-クロロ-1-[[2'-(1H-テトラゾール-5-イル)-1,1'-ビフェニル-4-イル]メチル]イミダゾール-5-メタノールカリウム;ロサルタン カリウム;ロサルタンカリウム塩;ロサルタン カリウム塩;ロサルタンカリウム (JP17)
英語化学名:
Losartan potassium
英語别名:
MK-95;COZAAR;MK 954;DUP 753;mk-0954;Aradois;l-158086;dupont753;thanolpotassium;DuP-753 potassium
CBNumber:
CB1442564
化学式:
C22H23ClKN6O
分子量:
462.01
MOL File:
124750-99-8.mol

ロサルタンカリウム 物理性質

融点 :
263-265°C
貯蔵温度 :
Desiccate at RT
溶解性:
Freely soluble in water and in methanol, slightly soluble in acetonitrile.
外見 :
powder or crystals
Merck :
14,5583
BRN :
5845770
InChIKey:
OXCMYAYHXIHQOA-UHFFFAOYSA-N
CAS データベース:
124750-99-8(CAS DataBase Reference)

安全性情報

主な危険性  Xi
Rフレーズ  36/37/38
Sフレーズ  26-36/37/39
WGK Germany  3
RTECS 番号 NI6755100
HSコード  2933290000
有毒物質データの 124750-99-8(Hazardous Substances Data)

ロサルタンカリウム 価格 もっと(15)

メーカー 製品番号 製品説明 CAS番号 包装 価格 更新時間 購入
富士フイルム和光純薬株式会社(wako) W01LKTL5873 ロサルタン カリウム塩
Losartan potassium
124750-99-8 1g ¥8100 2018-12-26 購入
富士フイルム和光純薬株式会社(wako) W01LKTL5873 ロサルタン カリウム塩
Losartan potassium
124750-99-8 5g ¥26100 2018-12-26 購入
東京化成工業 L0232 ロサルタンカリウム >98.0%(HPLC)(T)
Losartan Potassium >98.0%(HPLC)(T)
124750-99-8 5g ¥12800 2018-12-04 購入
東京化成工業 L0232 ロサルタンカリウム >98.0%(HPLC)(T)
Losartan Potassium >98.0%(HPLC)(T)
124750-99-8 25g ¥45000 2018-12-04 購入
Sigma-Aldrich Japan 1370462 ロサルタンカリウム United States Pharmacopeia (USP) Reference Standard
Losartan potassium United States Pharmacopeia (USP) Reference Standard
124750-99-8 150mg ¥70600 2018-12-25 購入

ロサルタンカリウム 化学特性,用途語,生産方法

外観

白色の結晶性の粉末で、味は苦い

溶解性

水:1g/ml以上、DMF:1g/ml以上、メタノール:約500mg/ml、エタノール:約400mg/ml、アセトニトリル:約2mg/ml、エーテルに不溶

用途

アンジオテンシンⅡ受容体拮 抗剤です。アンジオテンシンⅡ受容体タイプ Ⅰ( AT1)受容体に作用を示します。

用途

アンジオテンシンⅡ受容体拮 抗剤です。アンジオテンシンⅡ受容体タイプ Ⅰ(AT1)受容体に作用を示します。

効能

血圧降下薬, アンジオテンシンII受容体拮抗薬

商品名

ニューロタン (MSD)

説明

Losartan potassium is the first potent and selective non-peptide angiotensin II (AT II) AT1 receptor antagonist introduced to the market as a once-daily oral antihypertensive. It is efficacious and long lasting in controlling blood pressure in spontaneous hypertensive rats, in patients with essential hypertension in addition to those patients with renal impairment. Since losartan functions by competitive antagonism at the level of receptor, which represents the most direct way of selectively inhibiting the renin-angiotensin system (RAS) independent of the source of AT II, its use has been reported to be free of the coughing side effect exhibited by the ACE inhibitors. In contrast to calcium channel blockers, losartan does not appear to cause ankle edema, headache and tachycardia. It is also reported to be in clinical trials for the treatment of heart failure. Other reports indicate that losartan may have potential efficacy as an anxiolytic, an antiglaucoma agent, in addition to in providing protection against stroke and in preventing the myointimal proliferative response of the vascular wall after coronary angioplasty and surgery.

化学的特性

White to Off-White Crystalline Powder

Originator

DuPont Merck (U.S.A.)

使用

A nonpeptide angiotensin II AT1-receptor antagonist. Antihypertensive.

使用

antihypertensive, AT1 angiotensin II antagonist

使用

Coronary vasodilator used in the diagnosis of coronary heart disease (adenosine A2A agonist).

Manufacturing Process

2-Butyl-4-chloro-1-(2'-(tetrazol-5-yl)biphenyl-4-ylmethyl)-1H-imidazole-5- methanolpotassium was synthesized in 5 stages.
1. Methyl 4'-methylbiphenyl-2-carboxylate (44.2 mmol), 0.5 N KOH in methanol (133 mmol), and water (50 mL) were mixed and refluxed under nitrogen. After 5 hours, the solvent was removed in vacuo and water (200 mL) and ethyl acetate (200 mL) added. The aqueous layer was acidified with concentrated hydrochloric acid to a pH of 3 and the layers were separated. The aqueous phase was extracted with ethyl acetate, the organic layers collected, dried (MgSO4) and the solvent removed in vacuo to yield 8.71 g of a 4'-methylbiphenyl-2-carboxylic acid, melting point 140.0-145.0°C.
2. 4'-Methylbiphenyl-2-carboxylic acid (41 mmol) and thionyl chloride (411 mmol) were mixed and refluxed for 2 hours. The excess thionyl chloride was removed in vacuo and the residue was taken up in toluene. The toluene was removed by rotary evaporation. The crude acid chloride was then added slowly to cold (0°C) concentrated NH4OH (50 mL) so that the temperature was kept below 15°C. After 15 minutes of stirring, water (100 mL) was added and solids precipitated. These were collected, washed with water and dried under high vacuum over P2O5 to yield 7.45 g of a white solid, melting point 126.0-128.5°C. The above product amide (35 mmol) and thionyl chloride (353 mmol) were mixed and refluxed for 3 hours. The thionyl chloride was removed using the same procedure as described above. The residue was washed with a little hexane to yield 6.64 g of 4'-methyl-2-cyanobiphenyl, melting point 44.0- 47.0°C.
3. 4'-Methyl-2-cyanobiphenyl (5.59 g) was brominated using benzoyl peroxide as an initiator. The product was recrystallized from ether to yield 4.7 g of 4'- bromomethyl-2-cyanobiphenyl, melting point 114.5-120.0°C.
4. 4'-Bromomethyl-2-cyanobiphenyl (4.6 g) was alkylated onto 2-n-butyl-4- chloro-5-(hydroxymethyl)-imidazole. For separation of the product was used a flash chromatography in 1:1 hexane/ethyl acetate over silica gel. The regioisomeric products yielded 2.53 g of the faster eluting isomer. Recrystallization from acetonitrile yielded 1.57 g of analytically pure 2-n-butyl4-chloro-1-[2'-cyanobiphenyl-4-yl)methyl]-5-(hydroxymethyl)-imidazole, melting point 153.5 -155.5°C.
5. 2-n-Butyl-4-chloro-1-[(2'-cyanobiphenyl-4-yl)-methyl]-5-(hydroxymethyl)- imidazole (10 mmole), sodium azide (10 mmol), and ammonium chloride (30 mmol) were mixed in DMF (150 mL) under N2 at 100°C for 2 days, after which the temperature was raised to 120°C for 6 days. The reaction was cooled and 3 more equivalents each of ammonium chloride and sodium azide were added. The reaction was again heated for 5 days at 120°C. The reaction was cooled, the inorganic salts filtered, and the filtrate solvent removed in vacuo. Water (200 mL) and ethyl acetate (200 mL) were added to the residue and the layers were separated. The aqueous layer was extracted with ethyl acetate, the organic layers were collected, dried (MgSO4) and the solvent removed in vacuo, to yield a dark yellow oil. The product was purified by flash chromatography in 100% ethyl acetate to 100% ethanol over silica gel to yield 5.60 g of a light yellow 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1Htetrazol-5-yl)biphenyl-4-yl)methyl]imidazole. Recrystallization from acetonitrile yielded 4.36 g of light yellow crystals which still melted broadly. The crystals were taken up in 100 mL of hot acetonitrile. The solid that did not dissolve was filtered off to yield 1.04 g of product as a light yellow solid, melting point of 2-n-butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4- yl)methyl]imidazole 183.5-184.5°C.
2-n-Butyl-4-chloro-5-hydroxymethyl-1-[(2'-(1H-tetrazol-5-yl)biphenyl-4- yl)methyl]imidazole may be converted to potassium salt.

brand name

Cozaar (Merck).

Therapeutic Function

Antihypertensive

生物活性

Selective non-peptide angiotensin AT 1 receptor antagonist. Inhibits the contractile effects of angiotensin II on rabbit aorta and jugular vein (pA 2 = 8.27). Orally active antihypertensive agent.

ロサルタンカリウム 上流と下流の製品情報

原材料

準備製品


ロサルタンカリウム 生産企業

Global( 351)Suppliers
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Henan Tianfu Chemical Co.,Ltd.
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Hubei XinRunde Chemical Co., Ltd.
+8615102730682
02783214688 bruce@xrdchem.cn CHINA 568 55
Nanjing Finetech Chemical Co., Ltd.
025-85710122 17714198479
025-85710122 sales@fine-chemtech.com CHINA 890 55
ATK CHEMICAL COMPANY LIMITED
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+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24886 60
Hefei TNJ Chemical Industry Co.,Ltd.
86-0551-65418684 18949823763
86-0551-65418684 info@tnjchem.com China 2754 55
career henan chemical co
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QUALITY CONTROL CHEMICALS INC.
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Hebei Guanlang Biotechnology Co., Ltd.
+8619930501651
whatsapp: +8619930501651 breeduan@crovellbio.com CHINA 2586 58
hdzhl biotechnology co., ltd
86-13032617415
sales@luchibiology.com CHINA 1277 58

124750-99-8(ロサルタンカリウム)キーワード:


  • 124750-99-8
  • 2-BUTYL-4-CHLORO-1-[[2'-(1H-TETRAZOL-5YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1H-IMIDAZOLE-5-METHANOL
  • 2-butyl-4-chloro-1-[[2'-(1h-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1h-imidazole-5-methanol monopotassium salt
  • 2-BUTYL-4-CHLORO-1-[[2'-(1H-TETRAZOLE-5-YL)[1,1'-BIPHENYL]-4-YL]METHYL]-1H-IMIDAZOLE-5-METHANOL, POTASSIUM SALT
  • LOSARTAN MONOPOTASSIUM SALT
  • LOSARTAN POTASSIUM
  • LOSARTAN POTASSIUM SALT
  • MK 954
  • 1h-imidazole-5-methanol,2-butyl-4-chloro-1-((2’-(1h-tetrazol-5-yl)(1,1’-biphe
  • 2-butyl-4-chloro-1-(2’-(tetrazol-5-yl)biphenyl-4-ylmethyl)-1h-imidazole-5-me
  • COZAAR
  • DUP 753
  • Losartan PotassiuM (DuP 753)
  • Losartan Potassium (250 mg)
  • 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]Methyl]-1H-iMidaz
  • Losartan potassiuM API
  • 2-Butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)-1,1'-biphenyl-4-yl]methyl]imidazole-5-methanol Potassium Salt
  • Losartan PotassiuM/Losartan K
  • 2-butyl-4-chloro-1-[[2'-(2H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]-1H-imidazole-5-methanol, potassium salt (1:1)
  • potassium (1-((2'-(2H-tetrazol-5-yl)-[1,1'-biphenyl]-4-yl)methyl)-2-butyl-4-chloro-1H-imidazol-5-yl)methanolate
  • potassium (2-butyl-4-chloro-1-{[2'-(2H-tetrazol-5-yl)biphenyl-4-yl]methyl}-1H-imidazol-5-yl)methanolate
  • potassium [2-butyl-5-chloro-3-[[4-[2-(2H-1,2,3,4-tetrazol-5-yl)phenyl]phenyl]met
  • potassium [2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]-4-imidazolyl]methanolate
  • potassium [2-butyl-5-chloro-3-[[4-[2-(2H-tetrazol-5-yl)phenyl]phenyl]methyl]imidazol-4-yl]methanolate
  • potassium [2-butyl-5-chloro-3-[4-[2-(2H-tetrazol-5-yl)phenyl]benzyl]imidazol-4-yl]methanolate
  • Losartan Potassium (150 mg)
  • dupont753
  • l-158086
  • mk-0954
  • thanolpotassium
  • 2-butyl-4-chloro-1-[[2'-(1H-tetrazol-5-yl)[1,1'-biphenyl]-4-yl]methyl]- 1H-imidazole-5-methanol,monopotassium salt
  • 2-ブチル-4-クロロ-5-(ヒドロキシメチル)-1-[(2'-(1H-テトラゾール-5-イル)-1,1'-ビフェニル-4-イル)メチル]-1H-イミダゾール·カリウム塩
  • アラドイス
  • ロサルタンカリウム
  • 2-ブチル-4-クロロ-1-[[2'-(1H-テトラゾール-5-イル)-1,1'-ビフェニル-4-イル]メチル]-1H-イミダゾール-5-メタノール·カリウム
  • ニューロタン
  • 2-ブチル-4-クロロ-1-[[2'-(1H-テトラゾール-5-イル)-1,1'-ビフェニル-4-イル]メチル]イミダゾール-5-メタノールカリウム
  • ロサルタン カリウム
  • ロサルタンカリウム塩
  • ロサルタン カリウム塩
  • ロサルタンカリウム (JP17)
  • アンギオテンシン拮抗薬
  • 降圧薬
  • 抗不整脈薬
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