81486-22-8

Basic information

• Product Name: NIPRADILOL
• Synonyms: NIPRADILOL;K 351;3,4-Dihydro-8-[2-hydroxy-3-[(1-methylethyl)amino]propoxy]-2H-1-benzopyran-3-ol 3-nitrate;Hypadil;Nipradolol;Nipranol;2H-1-Benzopyran-3-ol, 3,4-dihydro-8-(2-hydroxy-3-((1-methylethyl)amino)propoxy)-, 3-nitrate;3,4-Dihydro-8-(2-hydroxy-3-(isopropylamino)propoxy)-2H-1-benzopyran-3-ol 3-nitrate
• CAS NO: 81486-22-8
• Molecular Formula: C₁₅H₂₂N₂O₆
• Molecular Weight: 326.34
• Product Categories: API
• Mol File: 81486-22-8.mol
• Article Data: 5

Chemical Properties

• Melting Point: 110-122℃
• Boiling Point: 464.39°C (rough estimate)
• Flash Point: 256.186 °C
• Appearance: Colorless needle crystal
• Density: 1.1829 (rough estimate)
• Vapor Pressure: 8.12E-11mmHg at 25°C
• Refractive Index: 1.6280 (estimate)
• CAS DataBase Reference: NIPRADILOL(CAS DataBase Reference)
• NIST Chemistry Reference: NIPRADILOL(81486-22-8)
• EPA Substance Registry System: NIPRADILOL(81486-22-8)

Safety Data

• Hazardous Substances Data: 81486-22-8(Hazardous Substances Data)

Usage

Description

Nipradilol is a beta-blocker with vasodilatory activity. As an antihypertensive nipradilol decreases systemic/pulmonary arterial blood pressure, heart rate, cardiac output and left ventricular volume without causing tachycardia. Nipradilol is also reported to have antiangina activity in dogs.

Originator

Kowa (Japan)

Uses

Nipradolol is a β-adrenoceptor blocking agent with antihypertensive properties.?Nipradolol is used as an?anti-glaucomatous agent.

Brand name

Hypadil

InChI:InChI=1/C15H22N2O6/c1-10(2)16-7-12(18)8-21-14-5-3-4-11-6-13(23-17(19)20)9-22-15(11)14/h3-5,10,12-13,16,18H,6-9H2,1-2H3

Upstream product

• 81486-20-6 3,4-dihydro-8-hydroxy-3-nitroxy-2H-1-benzopyran 
• 75-31-0 isopropylamine 
• 81486-21-7 (2'S)-3,4-dihydro-8-(2,3-epoxypropoxy)-3-nitroxy-2H-1-benzopyran 
• 81486-21-7 (2'R)-3,4-dihydro-8-(2,3-epoxypropoxy)-3-nitroxy-2H-1-benzopyran 
• 81486-17-1 3,4-dihydro-3,8-dihydroxy-2H-1-benzopyran 
• 91520-03-5 2-(2-acetoxy-3-chloro)propyl-6-methoxyphenol 
• 91520-01-3 3,4-dihydro-3-hydroxy-8-methoxy-2H-1-benzopyran 
• 91520-02-4 2-(2,3-Epoxypropyl)-6-methoxyphenyl acetate 
• 91520-04-6 8-methoxy-3,4-dihydro-2H-1-benzopyran-3-yl acetate 
• 2173-78-6 2-Allyl-6-methoxyphenyl acetate 
• 81486-21-7 3,4-dihydro-8-(2,3-epoxy)propoxy-3-nitroxy-2H-1-benzopyran 

Downstream Products

• 100921-90-2 3,4-dihydro-8-<3'-(N-isopropyl-N-L-menthoxyacetyl)amino-2'-L-menthoxyacetyl>propoxy-3-nitroxy-2H-1-benzopyran 
• 100921-95-7 3,4-dihydro-8-<2'(R)-p-chlorobenzoyloxy-3'-(N-p-chlorobenzoyl-N-isopropyl)amino>propoxy-3(R)-nitroxy-2H-1-benzopyran 
• 100921-96-8 3,4-dihydro-8-<2'(S)-p-chlorobenzoyloxy-3'-(N-p-chlorobenzoyl-N-isopropyl)amino>propoxy-3(S)-nitroxy-2H-1-benzopyran 
• 100922-03-0 3,4-dihydro-3(R),8-bis(p-chlorobenzoyloxy)-2H-1-benzopyran 
• 100922-04-1 3,4-dihydro-3(S),8-bis(p-chlorobenzoyloxy)-2H-1-benzopyran 
• 100921-90-2 3,4-dihydro-8-<3'-(N-isopropyl-N-L-menthoxyacetyl)amino-2'(R)-L-menthoxyacetyl>propoxy-3(R)-nitroxy-2H-1-benzopyran 
• 100921-90-2 3,4-dihydro-8-<3'-(N-isopropyl-N-L-menthoxyacetyl)amino-2'(S)-L-menthoxyacetyl>propoxy-3(S)-nitroxy-2H-1-benzopyran 
• 100921-98-0 3,4-dihydro-8-<2'(S)-p-chlorobenzoyloxy-3'-(N-p-chlorobenzoyl-N-isopropyl)amino>propoxy-3(R)-nitroxy-2H-1-benzopyran 
• 100921-97-9 3,4-dihydro-8-<2'(R)-p-chlorobenzoyloxy-3'-(N-p-chlorobenzoyl-N-isopropyl)amino>propoxy-3(S)-nitroxy-2H-1-benzopyran 
• 100992-19-6 3,4-dihydro-8-<3'-(N-p-chlorobenzoyl-N-isopropyl)amino-2'(S)-hydroxy>propoxy-3(R)-nitroxy-2H-1-benzopyran 
• 100992-18-5 3,4-dihydro-8-<3'-(N-p-chlorobenzoyl-N-isopropyl)amino-2'(R)-hydroxy>propoxy-3(S)-nitroxy-2H-1-benzopyran 
• 100992-17-4 3,4-dihydro-8-<3'-(N-p-chlorobenzoyl-N-isopropyl)amino-2'(S)-L-menthoxyacetyloxy>propoxy-3(R)-nitroxy-2H-1-benzopyran 
• 100921-94-6 3,4-dihydro-8-<3'-(N-p-chlorobenzoyl-N-isopropyl)amino-2'(R)-L-menthoxyacetyloxy>propoxy-3(S)-nitroxy-2H-1-benzopyran 
• 86247-86-1 3,4-dihydro-3(RS)-hydroxy-8-(2'(RS)-hydroxy-3'-isopropylamino)propoxy-2H-1-benzopyran 

Relevant articles and documents

THERAPY FOR COMPLICATIONS OF DIABETES

A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelin A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.

Method for treating resistant hypertension

A method is provided for lowering blood pressure in a patient having clinically diagnosed resistant hypertension. The method comprises administering darusentan to the patient adjunctively with a baseline antihypertensive regimen that comprises administration of at least one diuretic and at least two antihypertensive drugs selected from at least two of (a) ACE inhibitors and angiotensin II receptor blockers, (b) beta-adrenergic receptor blockers and (c) calcium channel blockers. The darusentan is orally administered at a dose and frequency effective, in combination with the baseline regimen, to provide a reduction of at least about 3 mmHg in one or more blood pressure parameters selected from trough sitting systolic, trough sitting diastolic, 24-hour ambulatory systolic, 24-hour ambulatory diastolic, maximum diurnal systolic and maximum diurnal diastolic blood pressures.

Synthesis and hypotensive activity of benzopyran derivatives

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