Synthesis of a Key Intermediate for the Preparation of FTY720 Analogs

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...

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Veröffentlicht in:	Chemical & pharmaceutical bulletin 2012/11/01, Vol.60(11), pp.1395-1398
Hauptverfasser:	Hamada, Maiko, Adachi, Kunitomo, Hikawa, Hidemasa, Yokoyama, Yuusaku
Format:	Artikel
Sprache:	eng
Schlagworte:	Alkynes - chemical synthesis Alkynes - chemistry Benzene Derivatives - chemical synthesis Benzene Derivatives - chemistry Catalysis chemoselectivity cross-coupling fingolimod Fingolimod Hydrochloride Immunosuppressive Agents - chemical synthesis Immunosuppressive Agents - chemistry KRP-203 palladium Palladium - chemistry Propylene Glycols - chemical synthesis Propylene Glycols - chemistry Sphingosine - analogs & derivatives Sphingosine - chemical synthesis Sphingosine - chemistry Sulfhydryl Compounds - chemical synthesis Sulfhydryl Compounds - chemistry
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