143228-85-7

Basic information

• Product Name: (S)-Azelastine
• Synonyms: (S)-4-[(4-Chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-1(2H)-phthalazinone;(S)-Azelastine;1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-(hexahydro-1-methyl-1H-azepin-4-yl)-, (S)-;1(2H)-Phthalazinone, 4-[(4-chlorophenyl)methyl]-2-[(4S)-hexahydro-1-methyl-1H-azepin-4-yl]-;(S)-Azelastine Hydrochloride 1
• CAS NO: 143228-85-7
• Molecular Formula: C22H24ClN3O
• Molecular Weight: 381.9
• Product Categories: Intermediates & Fine Chemicals;Pharmaceuticals
• Mol File: 143228-85-7.mol
• Article Data: 6

Chemical Properties

• Appearance: /
• CAS DataBase Reference: (S)-Azelastine(CAS DataBase Reference)
• NIST Chemistry Reference: (S)-Azelastine(143228-85-7)
• EPA Substance Registry System: (S)-Azelastine(143228-85-7)

Safety Data

• Hazardous Substances Data: 143228-85-7(Hazardous Substances Data)

Upstream product

• 58581-89-8 azelastine 
• 613-94-5 benzoic acid hydrazide 
• 53242-76-5 2‐(4-chlorophenylacetyl)benzoic acid 
• 110406-94-5 C₁₄H₂₁N₃O 
• 79307-93-0 azelastine hydrochloride 
• 105279-16-1 (Z)-3-(4-chlorophenyl)methylidenephthalide 
• 85-44-9 phthalic anhydride 
• 1859-33-2 1-methyl-1,2,3,5,6,7-hexahydroazepin-4-one 
• 1878-66-6 4-chlorophenylacetic Acid 
• 117078-69-0 2-Benzoyl-1-(hexahydro-1-methyl-1H-azepin-4-yl)hydrazin-hydrochlorid 
• 53242-88-9 4-[(4-chlorophenyl)methyl]-1(2H)-phthalazinone 
• 56824-22-7 2-(2-chloroethyl)-1-methylpyrrolidine hydrochloride 

Downstream Products

• 79307-93-0 azelastine hydrochloride 
• 1346617-06-8 C₂₂H₂₄ClN₃O₂ 
• 1346617-06-8 C₂₂H₂₄ClN₃O₂ 

Relevant articles and documents

Synthesis and structure of azelastine-N-oxides

Azelastine is among the most frequently used drugs; however, knowledge and solid data about its metabolites are scarcely found in literature. Thus, microsomal oxidation of azelastine is thought to produce the corresponding N-oxides, However, until now these products had never been produced in significant amounts. By oxidation of azelastine with H2O2, these N-oxides were now prepared in racemic form for the first time and were fully characterized. Their structure was additionally confirmed by a single crystal X-ray analysis. Both N-oxides were found to be non-cytotoxic in SRB assays.

A protein-based mixed selector chiral monolithic stationary phase in capillary electrochromatography

A new mixed selector chiral stationary phase (CSP) was prepared with co-immobilized human serum albumin and cellulase on a poly(glycidylmethacrylate-co-ethylene glycol dimethacrylate) (poly(GMA-co-EDMA)) monolith and the evaluation of its usefulness in chiral separation research was presented. For comparison, two single selector chiral stationary phases (CSPs) were also fabricated with the corresponding proteins. The enantioseparation ability of these CSPs was investigated by capillary electrochromatography (CEC) with various racemates. The mixed selector CSP exhibited a broader range of enantioselectivities than the single selectors and it could separate 10 chiral analytes while the two single selector CSPs resolved 3 and 8 respectively. Moreover, for (±)-warfarin, the enantioresolution was improved on the mixed selector CSP. Meanwhile, compared with the single selector CSPs, no additional preparation stage or reagent consumption was required in the simultaneous immobilization of different proteins, which is more favorable from economical and practical points of view. Consequently, by mixing HSA and cellulase together, the composite column combines the enantioselectivities of both individual proteins, thus expanding their application range practically.

Crystalline form of azelastine

Polymorph I of azelastine of formula (I), its preparation process which comprises the following steps: a) crystallizing azelastine from a solution of said compound in isobutylmethylketone; b) isolating the polymorph I of azelastine that appears in the prior step; and c) removing the organic solvent from the polymorph I of azelastine thus obtained, and its use as antihistamine.