153408-27-6

Basic information

• Product Name: azelastine hydrochloride
• Synonyms: 1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, monohydrochloride, (S)-;(S)-Azelastine Hydrochloride;(S)-4-[(4-Chlorophenyl)Methyl]-2-(hexahydro-1-Methyl-1H-azepin-4-yl)-1(2H)-phthalazinone Hydrochloride;Azelastine Impurity;(S)-Azelastine Hydrochloride 2
• CAS NO: 153408-27-6
• Molecular Formula: C22H24ClN3O·HCl
• Molecular Weight: 0
• EINECS: 253-720-4
• Product Categories: Aromatics;Chiral Reagents;Heterocycles;Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 153408-27-6.mol
• Article Data: 3

Chemical Properties

• Melting Point: 219-221?C
• Appearance: /
• Storage Temp.: -20°C Freezer
• Solubility: Chloroform (Slightly), Methanol (Slightly)
• CAS DataBase Reference: azelastine hydrochloride(CAS DataBase Reference)
• NIST Chemistry Reference: azelastine hydrochloride(153408-27-6)
• EPA Substance Registry System: azelastine hydrochloride(153408-27-6)

Safety Data

• Hazardous Substances Data: 153408-27-6(Hazardous Substances Data)

Usage

Description

Azelastine hydrochloride is an orally active H1-histamine receptor antagonist, which is a white solid in its chemical form. It is primarily known for its antihistaminic properties, making it a valuable compound in the pharmaceutical industry.

Uses

Used in Pharmaceutical Industry:
Azelastine hydrochloride is used as an antihistamine for the treatment of allergic rhinitis and other related conditions. It works by blocking the action of histamine, a substance in the body that causes allergic symptoms such as itching, redness, and swelling.
Used in Allergy Treatment:
Azelastine hydrochloride is used as a medication for the relief of symptoms associated with allergic reactions, such as sneezing, runny nose, and itchy eyes. Its antihistaminic properties help to alleviate these symptoms by inhibiting the effects of histamine on the body.
Used in Nasal Sprays:
Azelastine hydrochloride is also used as an active ingredient in nasal sprays for the treatment of nasal congestion and inflammation caused by allergies. The nasal spray formulation allows for direct application to the affected area, providing rapid relief from allergy symptoms.

InChI:InChI=1/C22H24ClN3O.ClH/c1-25-13-4-5-18(12-14-25)26-22(27)20-7-3-2-6-19(20)21(24-26)15-16-8-10-17(23)11-9-16;/h2-3,6-11,18H,4-5,12-15H2,1H3;1H/t18-;/m1./s1

Upstream product

• 1859-33-2 1-methyl-1,2,3,5,6,7-hexahydroazepin-4-one 
• 110406-94-5 C₁₄H₂₁N₃O 
• 58581-89-8 azelastine 
• 613-94-5 benzoic acid hydrazide 

Downstream Products

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

Relevant articles and documents

Preparation method of azelastine hydrochloride

The invention relates to the technical field of synthesis of raw material medicines, and particularly discloses a preparation method of azelastine hydrochloride. The method comprises the following steps: condensing benzoyl hydrazine and 1-methylhexahydroazepine-4-one serving as raw materials, reducing with sodium borohydride, and reacting to obtain a compound 1; preparing a solid intermediate compound 2 from the compound 1 and organic binary weak acid; hydrolyzing the compound 2, and cyclizing with a compound 3 to form a compound 4; and salifying the compound 4 by hydrochloric acid, and separating water by toluene to obtain a compound 5, namely azelastine hydrochloride. The intermediate compound 2 prepared by the invention is a solid, the stability of the intermediate compound 2 is greatly improved compared with that of hydrochloride obtained in other literatures, the intermediate compound 2 is free of hygroscopicity, the purity can reach 99% or above, the quality risk of subsequent bulk drugs can be greatly reduced, and the process production operation space is larger; and the obtained azelastine hydrochloride does not contain water and meets related quality standards, the yield is increased to 80% or above compared with other literatures, and the purity can reach 99% or above.

Use of combinations comprising non-sedating antihistamines and alpha-adrenergic drugs for the topical treatment of rhinitis/conjunctivitis and cold, cold-like and/or flu symptoms

Pharmaceutical combination, applicable topically, containing a non-sedating antihistamine in combination with an α-adrenergic agonist and optionally conventional physiologically acceptable carriers, diluting agents and auxiliaries substances for the prophylaxis and treatment of allergic and/or vasomotoric rhinitis, conjunctivitis, cold, cold-like and/ or flu symptoms are claimed.