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Synthesis 2013; 45(24): 3399-3403
DOI: 10.1055/s-0033-1340008
DOI: 10.1055/s-0033-1340008
paper
A Simple Synthesis of the Novel Antihistaminic Drug Olopatadine Hydrochloride
Further Information
Publication History
Received: 04 July 2013
Accepted after revision: 18 September 2013
Publication Date:
23 October 2013 (online)
Abstract
A new alternative route for the synthesis of olopatadine is described. The present strategy involves a Lewis acid mediated ring opening of a cyclic ether to introduce 3-(dimethylamino)propylidene group as the side chain.
Supporting Information
- for this article is available online at http://www.thieme-connect.com/ejournals/toc/synthesis. Included are copies of 1H and 13C NMR spectra for all new compounds and the HPLC chromatogram of 2.
- Supporting Information
-
References
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- 10 Recrystallization details: after two recrystallization using PE–EtOAc (9:1) system, compound 2 with E/Z = 2:3 ratio could be improved to E/Z = 1:9 ratio.
For synthetic processes, see: