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Chemical and Pharmaceutical Bulletin
Vol. 60 (2012) No. 11 p. 1395-1398

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http://doi.org/10.1248/cpb.c12-00477

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A concise synthesis of a useful intermediate 10 for the preparation of fingolimod (FTY-720) analogs was achieved by utilizing a chemoselective Sonogashira reaction of trihalobenzene 12 with alkyne 13. The reaction proceeded with high selectivity to give alkyne 11 containing the dihalobenzene moiety in good yield. Compound 11 was converted into intermediate 10 by hydrogenation without reduction of the halogen atoms.

Copyright © 2012 The Pharmaceutical Society of Japan

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