2,4-Dibromo-3A,7A-Dihydroindenone置于pentacarbonyliron体系中,用 Xylene 用作溶剂,化学反应 8.0H,以38%的收率获得4-溴-1-茚酮 参考文献:Luh,Tien-Yau; Lai,Chi Hung; Tam,Shang Wai,Journal Of The Chemical Society. Perkin Transactions I,1980,P. 444-447 标题:Luh,Tien-Yau; Lai,Chi Hung; Tam,Shang Wai,Journal Of The Chemical Society. Perkin Transactions I,1980,P. 444-447
专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-9394264-B2 优先权日:2009-11-13 标 题:Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA 权利人:RECEPTOS INC 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
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-8507538-B2 优先权日:2009-11-13 标 题:Selective heterocyclic sphingosine 1 phosphate receptor modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM RICHARD 权利人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM RICHARD; RECEPTOS INC 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-9481659-B2 优先权日:2011-05-13 标 题 :Selective heterocyclic sphingosine 1 phosphate receptor modulators 发明人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM RICHARD 权利人:BOEHM MARCUS F; MARTINBOROUGH ESTHER; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TAMIYA JUNKO; HUANG LIMING; YEAGER ADAM RICHARD; CELGENE INT II SÀRL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:BR-122018077504-B1 优先权日:2009-11-13 标题 :METHODS FOR SYNTHESIS OF SELECTIVE SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS
参考标题:Cu-Catalyzed Coupling Of Indanone Oxime Acetates With Thiols To 2,3-Difunctionalized Indenones 作者:Yuanyuan Fu,Xueyan Zhao,Dengfeng Chen,Jinyue Luo,Shenlin Huang 摘要:A Cu-Catalyzed Coupling Reaction Of Indanone Oxime Acetates With Thiols Has Been Developed For The Synthesis Of 2,3-Functionalized 1-Indenones. This Protocol Has Several Features Including Easy Mild Reaction Conditions, Stabilized Enamine Products, Good Tolerance Of Functional Groups, And No External Oxidants. This Reaction Enables Direct Derivatization On The Indanone Ring To Provide Valuable Functionalized
合成参考文献
摘要:Glushkov, V. A.; Shklyaev, Yu. V., Science of Synthesis Knowledge Updates, (2018) 3, 281.