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A Practical Synthesis of a Key Intermediate of Beraprost

Hao-ting Zhu,Yang He,Li Zhan,Ting Liu, Shi-qiong Yang, Li-tao Kang,Yu Luo

JOURNAL OF CHEMICAL RESEARCH(2018)

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摘要
A practical eight-step synthesis of a key intermediate of beraprost is described. The tricyclic cyclopent[b]benzofuran core can be prepared from 2,6-dibromo-4-chlorophenol. The butyric side chain is introduced by ortho-selective metal-halogen exchange and subsequent coupling with 4-(benzyloxy)butanal. The procedure is operationally simple and amenable to scale-up synthesis.
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关键词
synthesis of beraprost,prostacyclin,metal-halogen exchange,cyclopent[b]benzofuran
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