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A concise synthesis of Fingolimod: an orally available drug for treating multiple sclerosis
Ning Yan1, Kai Chen1, Xinfa Bai1
1School of Pharmacy, Yantai University, Yantai, Shandong 264005 China.
Abstract:
A concise route for the synthesis of Fingolimod is reported. Starting from n-octylbenzene and 3-nitropropionic acid, a sequence of reactions consisting of Friedel-Crafts acylation, reduction, and double Henry reaction, followed by hydrogenation were applied to prepare Fingolimod with a yield of 31%, and an overall atom economy of 82.7%. Graphical AbstractStarting from 3-nitropropanyl chloride, Fingolimod was obtained in 4 steps with an overall yield of 31%.
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