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Total Synthesis and Structural Determination of XR774, a Tyrosine Kinase Inhibitor

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Figshare2018-02-01 更新2026-04-29 收录
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https://figshare.com/articles/dataset/Total_Synthesis_and_Structural_Determination_of_XR774_a_Tyrosine_Kinase_Inhibitor/5845578
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Total synthesis and structural determination of XR774 has been accomplished. The benzo­[j]­fluoranthene skeleton has been constructed by regioselective coupling between tetraline 3 and tetralone 4 successively followed by the sequential transformation including the Birch reduction to prepare allylic alcohol, simultaneous bromination of vinylic and aromatic moieties, and the nickel-mediated intramolecular coupling reaction. The optical resolution of racemic 17 led to the first total synthesis of (−)-XR774.
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2018-02-01
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