Practical synthesis of methyl (E)-2-(3-(3-(2-(7-chloro-2-quinolinyl) ethenyl)phenyl)-3-oxopropyl)benzoate, a key intermediate of Montelukast
A novel and practical synthetic route is presented for the preparation of methyl-(E)-2-(3-(3-(2-(7-chloro-2-quinolinyl)ethenyl)phenyl)-3-oxopropyl) benzoate, the key intermediate of Montelukast, a leukotriene antagonist. The main diarylpropane framework was prepared via a polarity conversation reaction resulting in an acyl anion equivalent followed by a nucleophilic substitution reaction. The overall yield of this approach was 61%. This method is simple for operation and suitable for industrial production.
He, Liang,Guo, Yang Hui,Wang, Ya Ping,Wang, Xiang Jing,Zhang, Ji,Xiang, Wen Sheng
p. 518 - 520
(2012/06/16)
PROCESS FOR PREPARING A LEUKOTRIENE ANTAGONIST
Process for preparing montelukast or a pharmaceutically acceptable salt thereof, especially its sodium salt, that comprises the condensation of an aldehyde and 7-chloro-2-methylquinoline. Moreover, novel intermediates useful for the synthesis of montelukast are described as well as their preparation.
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Page/Page column 24
(2008/06/13)
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