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Updated: Feb 15, 2026

Pre-clinical Evaluation of Tyrosine Kinase Inhibitors for Treatment of Acute Leukemia
Published on: September 18, 2013
Total Synthesis and Structural Determination of XR774, a Tyrosine Kinase Inhibitor
Kuniaki Tatsuta1, Daisuke Sekine1, Shinichi Hayama1
1Department of Applied Chemistry, Faculty of Science and Engineering , Waseda University 3-4-1 Ohkubo , Shinjuku-ku, Tokyo 169-8555 , Japan.
Abstract:
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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