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ベタキソロール

ベタキソロール 化学構造式
63659-18-7
CAS番号.
63659-18-7
化学名:
ベタキソロール
别名:
1-[4-[2-(シクロプロピルメトキシ)エチル]フェノキシ]-3-[(1-メチルエチル)アミノ]-2-プロパノール;ベタキソロール;1-[4-[2-(シクロプロピルメトキシ)エチル]フェノキシ]-3-(イソプロピルアミノ)-2-プロパノール;1-[4-[2-(シクロプロピルメトキシ)エチル]フェノキシ]-3-イソプロピルアミノ-2-プロパノール
英語化学名:
Betaxolol
英語别名:
ZB-5;C06849;βxolol;BETAXOLOL;Betaxolols;Betoptic S;Betaxolol Base;Betaxolol, >=98%;Betaxolol USP/EP/BP;1-Isopropylamino-3-[4-(2-cyclopropylmethoxy-ethyl)phenoxy]-2-propanol
CBNumber:
CB1134548
化学式:
C18H29NO3
分子量:
307.43
MOL File:
63659-18-7.mol

ベタキソロール 物理性質

融点 :
61-63°C
沸点 :
448.0±40.0 °C(Predicted)
比重(密度) :
1.067±0.06 g/cm3(Predicted)
貯蔵温度 :
-20°C Freezer
酸解離定数(Pka):
pKa 9.21 (Uncertain)
CAS データベース:
63659-18-7(CAS DataBase Reference)

安全性情報

HSコード  29225090

ベタキソロール 価格 もっと(5)

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) W01TRCB328000 ベタキソロール
Betaxolol
63659-18-7 5mg ¥13800 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01TRCB328000 ベタキソロール
Betaxolol
63659-18-7 10mg ¥21300 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01TRCB328000 ベタキソロール
Betaxolol
63659-18-7 25mg ¥38800 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01TRCB328000 ベタキソロール
Betaxolol
63659-18-7 50mg ¥82500 2021-03-23 購入
富士フイルム和光純薬株式会社(wako) W01TRCB328000 ベタキソロール
Betaxolol
63659-18-7 100mg ¥145000 2021-03-23 購入

ベタキソロール 化学特性,用途語,生産方法

効能

抗緑内障薬, 血圧降下薬, β1遮断薬

化学的特性

White Crystalline Solid

Originator

Kerlone,Carriere,France,1983

使用

Cardioselective 1-adrenergic blocker. An antihypertensive; antiglaucoma

使用

Cardioselective β1-adrenergic blocker. An antihypertensive; antiglaucoma.

定義

ChEBI: A propanolamine that is 3-aminopropane-1,2-diol in which the hydrogen of the primary hydoxy is substituted by a 4-[2-(cyclopropylmethoxy)ethyl]phenyl group and one of the hydrogens attached to the amino group is substituted by isopropyl. It is a selective beta1-receptor blocker and is used in the treatment of glaucoma as well as hypertension, arrhythmias, and coronary heart disease. It is also used to reduce non-fatal cardiac events in patients with heart failure.

Manufacturing Process

(1) 1 g of sodium hydroxide pellets (0.025 mol) is added to a suspension of 3.8 g of 4-[2-(cyclopropylmethoxy)-ethyl]-phenol in 30 ml of water. When the solution becomes homogenous, 2.3 ml of epichlorohydrin are added and the mixture is stirred for 8 hours. It is then extracted with ether and the extract is washed with water, dried over sodium sulfate and evaporated to dryness. The compound is purified by passing it over a silica column. 2.4 g of 1-[4-[2- (cyclopropylmethoxy)ethyl]-phenoxy]-2,3-epoxy-propane are thus obtained.
(2) 4.9 g of the preceding compound (0.02 mol) are condensed with 25 ml of isopropylamine by contact for 8 hours at ambient temperature and then by heating for 48 hours at the reflux temperature. After evaporation to dryness, the compound obtained is crystallized from petroleum ether. 5 g (yield 80%) of 2-[[4-(2-cyclopropylmethoxy)-ethyl]-phenoxy]-3-isopropylaminopropan-2-ol are thus obtained, melting point 70° to 72°C.
The hydrochloride is prepared by dissolving the base in the minimum amount of acetone and adding a solution of hydrochloric acid in ether until the pH is acid. The hydrochloride which has precipitated is filtered off and is recrystallized twice from acetone, melting point 116°C.

brand name

Betoptic (Alcon); Kerlone (Sanofi Aventis).

Therapeutic Function

Beta-adrenergic blocker

Veterinary Drugs and Treatments

Betaxolol HCl is a specific Beta1 adrenergic blocking agent which reduces aqueous humor production by decreasing cyclic-AMP synthesis in the ciliary body. This drug is a suitable substitute for timolol and because of its specific Beta1 activity, might be a first choice Beta blocking agent for patients with concurrent respiratory disease. Either levobunolol HCl or betaxolol HCl would be the first choice Beta blocking agent in a feline patient with glaucoma and asthma, although a topical carbonic anhydrates inhibitor should be considered before a Beta blocking agent in this situation. Betaxolol and the other Beta blockers should be used with caution in patients with cardiac disease.

代謝

Absorption of an oral dose of betaxolol (Kerlone, Betoptic) is almost complete. The drug is subject to a slight first-pass effect such that the absolute bioavailability of the drug is about 90%.Approximately 50% of administered betaxolol binds to plasma proteins, and its plasma half-life is about 20 hours; it is suitable for dosing once per day.The primary route of elimination is by liver metabolism, with only 15% of unchanged drug being excreted.

ベタキソロール 上流と下流の製品情報

原材料

準備製品


ベタキソロール 生産企業

Global( 120)Suppliers
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63659-18-7(ベタキソロール)キーワード:


  • 63659-18-7
  • BETAXOLOL
  • 1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)-2-propan
  • 2-propanol,1-(4-(2-(cyclopropylmethoxy)ethyl)phenoxy)-3-((1-methylethyl)amino)
  • 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)-2-propanol
  • Betaxolols
  • (-1-(Isopropylamino)-3-[p-(cyclopropylmethoxyethyl)phenoxy]-2-propanol
  • 1-[4-(2-(Cyclopropylmethyloxy)ethyl]-phenoxy]-3-[(1-methylethyl)amino]-2-propa nol
  • 1-Isopropylamino-3-[4-(2-cyclopropylmethoxy-ethyl)phenoxy]-2-propanol
  • Betoptic S
  • 1-[4-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(propan-2-ylamino)propan-2-ol
  • 1-[4-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-(isopropylamino)-2-propanol
  • 1-[4-[2-(Cyclopropylmethoxy)ethyl]phenoxy]-3-isopropylamino-2-propanol
  • C06849
  • βxolol
  • Betaxolol Base
  • ZB-5
  • 1-[4-[2-(cyclopropylmethoxy)ethyl]phenoxy]-3-[(1-methylethyl)amino]-2-propanol
  • Betaxolol, >=98%
  • Betaxolol USP/EP/BP
  • 1-[4-[2-(シクロプロピルメトキシ)エチル]フェノキシ]-3-[(1-メチルエチル)アミノ]-2-プロパノール
  • ベタキソロール
  • 1-[4-[2-(シクロプロピルメトキシ)エチル]フェノキシ]-3-(イソプロピルアミノ)-2-プロパノール
  • 1-[4-[2-(シクロプロピルメトキシ)エチル]フェノキシ]-3-イソプロピルアミノ-2-プロパノール
  • βアドレナリン遮断薬
  • 降圧薬
  • 眼科用薬
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