Synthesis of a Key Intermediate for the Preparation of FTY720 Analogs

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概要

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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.

• 公益社団法人　日本薬学会の論文

著者

• Yokoyama Yuusaku

  School of Pharmaceutical Science, Toho University

• Hamada Maiko

  School of Pharmaceutical Science, Toho University

• Adachi Kunitomo

  Medicinal Chemistry Research Laboratories I, Research Division, Mitsubishi Tanabe Pharma Corporation

• Hikawa Hidemasa

  School of Pharmaceutical Science, Toho University

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