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:WO-2019058290-A1 优先权日:2017-09-20 标 题 :IMPROVED PROCESS FOR THE PREPARATION OF AZANIMOD A-AMINO COMPOUND 发明人:CHINNAPILLAI RAJENDIRAN; PERIYANDI NAGARAJAN; JASTI VENKATESWARALU 权利人:SUVEN LIFE SCIENCES LTD; CHINNAPILLAI RAJENDIRAN; PERIYANDI NAGARAJAN; JASTI VENKATESWARALU 摘要:The present invention relates to an improved process for the preparation of an optically active chiral amino compound. The present invention relates in particular to an improved process for the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile, an important intermediate for the synthesis of ozanimod. The present invention relates more particularly to the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile using 4-cyano-1-indanone and alpha-methylbenzylamine derivatives. as raw materials. The present invention particularly relates to the preparation of (S) -1-amino-2,3-dihydro-1H-indene-4-carbonitrile comprising a synthesis of diastereoselective chiral amine by protection with chiral auxiliary ï?¡-methyl benzylamine derivatives followed reduction and debenzylation.
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:US-2023002426-A1 优先权日:2019-11-15 标题 :Chiral synthesis of a tertiary alcohol
参考文献:10.1107/s1600536811016175 摘要:Lipińska TM, Karczmarzyk Z, Wysocki W, Gruba E, Fruziński A. 5,6,7,8-Tetra-hydro-quinolin-8-one. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1365.