Azelastine hydrochloride

Base Information

• Chemical Name: Azelastine hydrochloride
• CAS No.: 79307-93-0
• Molecular Formula: C22H24ClN3O.HCl
• Molecular Weight: 418.366
• Hs Code.: 2933992600
• European Community (EC) Number: 253-720-4,620-469-0
• NSC Number: 758971
• UNII: 0L591QR10I
• DSSTox Substance ID: DTXSID2045945
• Wikidata: Q27105897
• NCI Thesaurus Code: C47408
• RXCUI: 235824
• ChEMBL ID: CHEMBL1200809
• Mol file: 79307-93-0.mol

Synonyms:4-((4-chlorophenyl)methyl)-2- (hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)- phthalazinone HCl;4-(p-chlorobenzyl)-2-(N-methylperhydroazepinyl-(4))-1-(2H)-phthalazinone;A 5610;A-5610;Afluon;Allergodil;Astelin;azelastine;azelastine hydrochloride;Azeptin;Corifina;Loxin;Optilast;Optivar;Rhinolast;Vividrin akut Azelastin

Chemical Property of Azelastine hydrochloride

Chemical Property:

• Appearance/Colour: white crystalline powder
• Melting Point: 225-229 °C
• Boiling Point: 533.9 °C at 760 mmHg
• Flash Point: 276.7 °C
• PSA: 38.13000
• Density: 1.25 g/cm³
• LogP: 5.03740
• Storage Temp.: -20°C Freezer
• Solubility.: DMSO: >10mg/mL
• Hydrogen Bond Donor Count: 1
• Hydrogen Bond Acceptor Count: 3
• Rotatable Bond Count: 3
• Exact Mass: 417.1374678
• Heavy Atom Count: 28
• Complexity: 558

Purity/Quality:

99.5% ^*data from raw suppliers

Azelastine Hydrochloride ^*data from reagent suppliers

Safty Information:

• Pictogram(s): Xn
• Hazard Codes: Xn
• Statements: 22

MSDS Files:

SDS file from LookChem

Total 1 MSDS from other Authors

Useful:

• Canonical SMILES: CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl
• Recent ClinicalTrials: Efficacy and Safety Study of AI201901 in Allergic Rhinitis Patients
• Recent EU Clinical Trials: COVID-19: Reducing Symptoms and Hospitalization rates by use of Azelastine Nasal spray in patients suffering from COVID-19 in Early stages
• Description: Azelastine hydrochloride is an orally effective antihistamine useful in the treatment of asthma and nasal allergy. It appears to inhibit release of histamine, in addition to antagonizing its action.

Technology Process of Azelastine hydrochloride

There total 12 articles about Azelastine hydrochloride which guide to synthetic route it. The literature collected by LookChem mainly comes from the sharing of users and the free literature resources found by Internet computing technology. We keep the original model of the professional version of literature to make it easier and faster for users to retrieve and use. At the same time, we analyze and calculate the most feasible synthesis route with the highest yield for your reference as below:

synthetic route:

Reference yield: 87.0%

azelastine (58581-89-8,143228-85-7) → azelastine hydrochloride (79307-93-0,153408-27-6)

Guidance literature:

With hydrogenchloride; In toluene; Reflux;

Reference yield: 5.0%

→ azelastine hydrochloride (79307-93-0,153408-27-6)

Guidance literature:

Reference yield:

→ tetryzoline hydrochloride (522-48-5) + azelastine hydrochloride (79307-93-0,153408-27-6)

Guidance literature:

upstream raw materials:

1-methyl-1,2,3,5,6,7-hexahydroazepin-4-one

C₁₄H₂₁N₃O

azelastine

benzoic acid hydrazide

Downstream raw materials:

azelastine

2-(1-benzylazepan-4-yl)-4-(4-chlorobenzyl)phthalazin-1(2H)-one

Refernces

• 1、 -. "Azelastine hydrochloride-containing percutaneous preparation having good percutaneous absorbability and reduced skin irritation". . . Retrieved 2008/06/13.
• 2、 Marchetti,Sechi,Botteghi,Paganelli. "Preparation of pharmaceuticals by hydroformylation. Part III. The synthesis of N-(4-Pyridyl)-3,3-diphenyl-1-aminopropane (Phenpyramine, Milverine)". . p. 74 - 76. Retrieved 2007/10/03.