专利号:US-7452994-B2 优先权日:2001-09-12 标 题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings 发明人:MCEACHERN ERNEST J; BRIDGER GARY J; SKUPINSKA KRYSTYNA A; SKERLJ RENATO T; YANG WEN 权利人:ANORMED INC 摘要:This invention describes various processes for synthesis and resolution of racemic amino-substituted fused bicyclic ring systems. One process utilizes selective hydrogenation of an amino-substituted fused bicyclic aromatic ring system. An alternative process prepares the racemic amino-substituted fused bicyclic ring system via nitrosation. In addition, the present invention describes the enzymatic resolution of a racemic mixture to produce the (R)- and (S)-forms of amino-substituted fused bicyclic rings as well as a racemization process to recycle the unpreferred enantioner. Further provided by this invention is an asymmetric synthesis of the (R)- or (S)-enantiomer of primary amino-substituted fused bicyclic ring systems.
专利号:US-2003114679-A1 优先权日:2001-09-12 标 题:Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
专利号:US-2005080267-A1 优先权日:2001-09-12 标 题:Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
专利号:US-2007060757-A1 优先权日:2001-09-12 标题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
专利号:EP-1487795-A2 优先权日:2001-09-12 标题 :Synthesis of enantiomerically pure amino-substituted fused bicyclic rings
专利号:EP-1487795-A4 优先权日:2001-09-12 标题 :SYNTHESIS OF ENANTIOMERICALLY PURE AMINO-SUBSTITUTED FUSIONNATED BICYCLIC CORES
参考文献:10.1055/s-0040-1707236 摘要:Jin L, Hu X, Zong Z, Wu K, Sun N, Hu B, Shen Z. Large-Scale Synthesis of 2-Chlorotetrahydroquinoline and 2-Chlorotetrahydroquinolin-8-one. Synthesis. 2020 Aug 27;52(23):3675–83. doi: 10.1055/s-0040-1707236.