Acrivastine - CAS 87848-99-5
Category: Inhibitor
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Molecular Formula:
C22H24N2O2
Molecular Weight:
348.44
COA:
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Targets:
Histamine Receptor
Description:
Acrivastine, also known as BW825C, is an antihistamine with peripheral H1-antagonist potency equal to that of triprolidine for the treatment of allergic rhinitis.
Synonyms:
(E)-3-[6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic acid; acrivastine; BW 825C; BW-825C; BW825C; Glaxo Wellcome brand of acrivastine; GlaxoSmithKline brand of acrivastine; Semprex
Solubility:
DMSO: 10.45 mg/mL (Need ultrasonic)
Storage:
Store in a cool and dry place (or refer to the Certificate of Analysis).
MSDS:
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Boiling Point:
555.1±50.0 ℃ at 760 Torr
Melting Point:
222 ℃ (decomp)
Density:
1.170±0.06 g/cm3
InChIKey:
PWACSDKDOHSSQD-IUTFFREVSA-N
InChI:
1S/C22H24N2O2/c1-17-7-9-18(10-8-17)20(13-16-24-14-2-3-15-24)21-6-4-5-19(23-21)11-12-22(25)26/h4-13H,2-3,14-16H2,1H3,(H,25,26)/b12-11+,20-13+
Canonical SMILES:
CC1=CC=C(C=C1)C(=CCN2CCCC2)C3=CC=CC(=N3)C=CC(=O)O
1.Spectrofluorimetric determination of acrivastine in spiked human urine and pharmaceuticals.
Fernández R1, Bello MA, Callejón M, Jiménez JC, Guiraúm A. Talanta. 2002 Mar 4;56(3):571-6.
A spectrofluorimetric method to determine acrivastine is proposed and applied to its determination in human urine and pharmaceuticals. The fluorimetric method allows the determination of 58-2000 ng ml(-1) of acrivastine in aqueous solutions containing acetic acid-sodium acetate buffer (pH 6.5) with lambda(exc)=230 nm and lambda(em)=380 nm.
2.Chromatographic separation and spectroscopic characterization of the E/Z isomers of acrivastine.
Davadra PM1, Dabhi B, Singh MK, Jain MR, Joshi HS, Bapodra AH. Chirality. 2011 Nov;23(10):955-60. doi: 10.1002/chir.21022. Epub 2011 Sep 26.
A reverse phase high performance liquid chromatography (HPLC) method has been developed for the separation of two geometric isomers of Acrivastine using crude reaction mixture. The resolution between two isomers was found more than 2.9. The geometric isomers have been isolated by preparative HPLC and characterized by spectroscopic techniques, such as NMR, infrared, and MS. The developed method has been validated for the determination of Z-isomer in Acrivastine. The limit of detection and limit of quantification of the Z-isomer were 0.05 and 0.2 μg/ml, respectively. The developed method is precise, linear, accurate, rugged and robust for its intended use.
3.Small molecule analysis using laser desorption/ionization mass spectrometry on nano-coated silicon with self-assembled monolayers.
Çelikbıçak Ö1, Demirel G, Pişkin E, Salih B. Anal Chim Acta. 2012 Jun 4;729:54-61. doi: 10.1016/j.aca.2012.04.006. Epub 2012 Apr 12.
Matrix-assisted laser desorption/ionization mass spectrometry (MALDI-MS) is an emerging technique for the determination of the molecular weight of biomolecules and their non-covalent complexes without fragmentation. One problem with this technique is the use of excess amounts of matrices, which may produce intense fragment ions and/or clusters at low mass ranges between 1 and 800 Da. These fragments lead to interference, especially concerning the signals of small target molecules. Here, a simple, reusable, and quite inexpensive approach was demonstrated to improve the effectiveness of laser desorption/ionization mass spectrometry (LDI-MS) analysis, especially for small molecules, without using matrix molecules. In this study, substrates with controllable morphologies and thicknesses were developed based on the self-assembly of silane molecules on silicon surfaces using N-(3-trimethoxysilylpropyl)diethylenetriamine (TPDA) and octadecyltrichlorosilane (OTS) molecules.
4.Synthesis of aryl(di)azinyl ketones through copper- and iron-catalyzed oxidation of the methylene group of aryl(di)azinylmethanes.
De Houwer J1, Abbaspour Tehrani K, Maes BU. Angew Chem Int Ed Engl. 2012 Mar 12;51(11):2745-8. doi: 10.1002/anie.201108540. Epub 2012 Jan 30.
Sustainable Oxidations: an oxidation method to transform aryl(di)azinylmethanes into aryl(di)azinyl ketones is described. Base metals (copper and iron) as catalysts in combination with O(2) as the oxidant are used, which makes this method sustainable. The utility of this method is illustrated by the synthesis of 6-(4-methylbenzoyl)pyridine-2-carbaldehyde, which is an intermediate in the preparation of the drug Acrivastine.
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CAS 87848-99-5 Acrivastine

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