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Name	Azelastine hydrochloride	EINECS	200-306-6
CAS No.	79307-93-0	Density	1.25 g/cm³
PSA	38.13000	LogP	5.03740
Solubility	13 g/L at 20 °C (insoluble in ethanol, ether)	Melting Point	225-229 °C
Formula	C₂₂H₂₄ClN₃O.HCl	Boiling Point	533.9 °C at 760 mmHg
Molecular Weight	418.366	Flash Point	276.7 °C
Transport Information	N/A	Appearance	white crystalline powder
Safety		Risk Codes	22
Molecular Structure		Hazard Symbols	Xn
Synonyms	1(2H)-Phthalazinone,4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-,monohydrochloride (9CI);A 5610;Allergodil;Astelin;Astepro;Azeptin;E 0659;Optivar;Rhinolast;W 2979M;	Article Data	4

Azelastine hydrochloride Synthetic route

: 10273-89-9
2-(2-methylphenyl)pyridine

: 79307-93-0
azelastine hydrochloride

: C34H34N4O

Conditions

Conditions	Yield
With C17H24N5Ru(1+)*F6P(1-); potassium acetate; potassium carbonate In 1-methyl-pyrrolidin-2-one at 35℃; for 72h; Inert atmosphere; Glovebox;	90%

: 79307-93-0
azelastine hydrochloride

A: 7-oxo-azelastine

B: 2-oxo-azelastine

Conditions

Conditions	Yield
With water; iodine; sodium hydrogencarbonate In tetrahydrofuran at 20℃; for 4h; chemoselective reaction;	A 37% B 6%

: 79307-93-0
azelastine hydrochloride

: 58581-89-8
azelastine

Conditions

Conditions	Yield
With sodium hydroxide In water pH=10; Inert atmosphere;

: 79307-93-0
azelastine hydrochloride

: 103541-65-7
2-(1-benzylazepan-4-yl)-4-(4-chlorobenzyl)phthalazin-1(2H)-one

Conditions

Conditions	Yield
Multi-step reaction with 2 steps 1.1: sodium hydroxide / water / pH 10 / Inert atmosphere 2.1: tri(4-tolyl)aminium hexafluorophosphate; 1,4-diaza-bicyclo[2.2.2]octane / acetonitrile / -5 °C / Inert atmosphere 2.2: 0 °C / Inert atmosphere View Scheme

Azelastine hydrochloride Chemical Properties

Product Name: Azelastine hydrochloride (CAS NO: 79307-93-0)
IUPAC Name: 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)phthalazin-1-onehydrochloride

Molecular formula: C₂₂H₂₅Cl₂N₃O
Formula weight: 418.36
Melting point: 225-229°C
Flash Point: 276.7 °C
Enthalpy of Vaporization: 81 kJ/mol
Boiling Point: 533.9 °C at 760 mmHg
Vapour Pressure: 1.77E-11 mmHg at 25°C
Chemical synonyms: a5610 ; azeptin;e-0659 ; w-2979m ; 4-[(4-chlorophenyl)methyl]-2-(1-methylazepan-4-yl)-phthalazin-1-one hydrochloride ; 4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone Hydrochloride

Azelastine hydrochloride Toxicity Data With Reference

1.	orl-rat LD50:580 mg/kg	KSRNAM Kiso to Rinsho. Clinical Report. 20 (1986),5231.
2.	ivn-rat LD50:24,600 µg/kg	KSRNAM Kiso to Rinsho. Clinical Report. 20 (1986),5231.
3.	orl-mus LD50:143 mg/kg	KSRNAM Kiso to Rinsho. Clinical Report. 20 (1986),5231.
4.	ivn-mus LD50:25,400 µg/kg	KSRNAM Kiso to Rinsho. Clinical Report. 20 (1986),5231.
5.	orl-dog LD50:107 mg/kg	KSRNAM Kiso to Rinsho. Clinical Report. 20 (1986),5235.

Azelastine hydrochloride Safety Profile

Poison by ingestion and intravenous routes. An experimental teratogen. Other experimental reproductive effects. When heated to decomposition it emits toxic fumes of NO_x and HCl.

Azelastine hydrochloride Specification

Side effects of azelastine nasal spray vary somewhat depending on the condition being treated. The most common side effects include bitter taste, headache, rhinitis, nose bleed, and somnolence. Adults being treated for vasomotor rhinitis may also experience dysesthesia and sinusitis. Additional side effects experienced by adults being treated for seasonal allergies include nasal burning, pharyngitis, dry mouth, paroxysmal sneezing, nausea, fatigue, dizziness, and weight gain. Additional side effect can include a slight mind alertness.

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