74191-85-8

  • Product Name:Doxazosin
  • Molecular Formula:C23H25N5O5
  • Purity:99%
  • Molecular Weight:451.482
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Product Details;

CasNo: 74191-85-8

Molecular Formula: C23H25N5O5

Chinese Manufacturer Supply Doxazosin, Factory Sells 74191-85-8 with Competitive Price

  • Molecular Formula:C23H25N5O5
  • Molecular Weight:451.482
  • Vapor Pressure:1.83E-20mmHg at 25°C 
  • Melting Point:289-290 °C 
  • Boiling Point:718 °C at 760 mmHg 
  • PKA:6.52±0.50(Predicted) 
  • Flash Point:388 °C 
  • PSA:175.02000 
  • Density:1.371 g/cm3 
  • LogP:2.88670 

Doxazosin (Cas 74191-85-8) Usage

Description

Doxazosin mesylate is a selective alpha, blocker indicated for the treatment of hypertension, reportedly of special benefit as a first-line agent in the most hypertonic patient population. Another advantage of doxazosin is its favorable effect on blood lipids; it significantly increases the HDL/total cholesterol ratio and decreases the total cholesterol as well as triglycerides levels.

Originator

Pfizer (United Kingdom)

Uses

ACIPHEX therapeutic Erosive or Ulcerative Gastroesophageal Reflux Disease. Doxazosin has also been used successfully in combination with β-adrenoceptor antagonists, diuretics, calcium channel antagonists, and angiotensin-converting enzyme inhibitors in patients with hypertension that is uncontrolled with monotherapy.

Definition

ChEBI: A member of the class of quinazolines that is quinazoline substituted by an amino group at position 4, methoxy groups at positions 6 and 7 and a piperazin-1-yl group at position 2 which in turn is substituted by a 2,3-dihydro-1,4-benzodioxin-2-ylcarbonyl roup at position 4. An antihypertensive agent, it is used in the treatment of high blood pressure.

Brand name

Cardura (Pfizer);Carduran.

General Description

Doxazosin, 1-(4-amino-6,7-dimethoxy-2-quinazolinyl)-4-(1,4-benzodioxan-2-ylcarbonyl)piperazine(Cardura), is a quinazoline compound that selectively inhibitsthe α1-subtype of α-adrenergic receptors. This agentis very useful in the management of hypertension associatedwith pheochromocytoma.

Clinical Use

Alpha-adrenoceptor blocker:HypertensionBenign prostatic hyperplasia (BPH)

Drug interactions

Potentially hazardous interactions with other drugsAntidepressants: enhanced hypotensive effect with MAOIs.Avanafil, vardenafil, sildenafil and tadalafil: enhanced hypotensive effect, avoid with tadalafil, start the others at the lowest possible dose.Beta-blockers: enhanced hypotensive effect; increased risk of first dose hypotensive effect.Calcium-channel blockers: enhanced hypotensive effect, increased risk of first dose hypotensive effect.Diuretics: enhanced hypotensive effect, increased risk of first dose hypotensive effect.Moxisylyte: possibly severe postural hypotension when used in combination.

Metabolism

Doxazosin is extensively metabolised in the liver, and excreted in faeces as inactive metabolites (6-hydroxydoxazosin) and a small amount of unchanged drug

InChI:InChI=1/C23H25N5O5.CH4O3S/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20;1-5(2,3)4/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26);1H3,(H,2,3,4)

74191-85-8 Relevant articles

Doxazosin in the Treatment of Benign Prostatic Hyperplasia in Normotensive Patients: A Multicenter Study

Ahmed Fawzy, Karl Braun, George P. Lewis, Michael Gaffney, Kathleen Ice, and Norma Dias for the Multicenter Study Group

, Journal of UrologyClinical Urology: Original Article1 Jul 1995

Adverse events, primarily mild to moderate in severity, were reported in 44 percent of patients given doxazosin and 30 percent of those given placebo. Our results strongly demonstrate that doxazosin is significantly superior to placebo in the treatment of BPH in normotensive patients, with the patient experiencing significant relief early after initiation of therapy.

Process for the Preparation of Doxazosin and Salts Thereof

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, (2012/03/08)

The present invention relates to a proce...

THERAPY FOR COMPLICATIONS OF DIABETES

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, (2009/07/02)

A method for enhancing glycemic control ...

ANTIHYPERTENSIVE THERAPY

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, (2009/09/08)

A new use of darusentan is provided in p...

74191-85-8 Process route

1,4-benzodioxane-2-carboxylic acid
3663-80-7,34385-93-8,70918-53-5,70918-54-6

1,4-benzodioxane-2-carboxylic acid

4-amino-6,7-dimethoxy-2-piperazin-1-ylquinazoline
60547-97-9

4-amino-6,7-dimethoxy-2-piperazin-1-ylquinazoline

doxazosin
74191-85-8,104874-86-4,70918-17-1

doxazosin

Conditions
Conditions Yield
With 1,1'-carbonyldiimidazole; In tetrahydrofuran; at 0 - 20 ℃; for 5.16667h;
80%
2-chloro-6,7-dimethoxyquinazolin-4-amine
23680-84-4

2-chloro-6,7-dimethoxyquinazolin-4-amine

(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)(piperazin-1-yl)methanone
70918-00-2

(2,3-dihydrobenzo[b][1,4]dioxin-2-yl)(piperazin-1-yl)methanone

doxazosin
74191-85-8,104874-86-4,70918-17-1

doxazosin

Conditions
Conditions Yield
In butan-1-ol; Reflux;
88%
In butan-1-ol; for 5h; Heating;
83%

74191-85-8 Upstream products

  • 23680-84-4
    23680-84-4

    2-chloro-6,7-dimethoxyquinazolin-4-amine

  • 70918-00-2
    70918-00-2

    (2,3-dihydrobenzo[b][1,4]dioxin-2-yl)(piperazin-1-yl)methanone

  • 4739-94-0
    4739-94-0

    ethyl 2,3-dihydro-1,4-benzodioxin-2-carboxylate

  • 120-80-9
    120-80-9

    benzene-1,2-diol

74191-85-8 Downstream products

  • 156154-10-8
    156154-10-8

    doxazosin mesylate

  • 156154-10-8
    156154-10-8

    doxazosin mesylate

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