📜3-氰基-4-异丙氧基苯甲酸置于三甲基硅醇,Potassium Trimethylsilonate,N,N'-羰基二咪唑体系中,用 四氢呋喃,N-甲基吡咯烷酮 用作溶剂,化学反应 21.5H,反应生成奥扎莫德 参考文献: Improved Process For Preparing Ozanimod[fr] Procédé Amélioré Pour La Préparation D'Ozanimod 标题: Improved Process For Preparing Ozanimod[fr] Procédé Amélioré Pour La Préparation D'Ozanimod 摘要:所提出的发明涉及制备公式(1)的化合物或其盐的过程(即ozanimod):(1).该发明还涉及用于该过程的中间体.
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: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-10906888-B2 优先权日:2016-07-14 标 题:Pyrimidine carboxamides as inhibitors of Vanin-1 enzyme 发明人:CASIMIRO-GARCIA AGUSTIN; STROHBACH JOSEPH WALTER; HEPWORTH DAVID; LOVERING FRANK ELDRIDGE; CHOI CHULHO; ALLAIS CHRISTOPHE PHILIPPE; WRIGHT STEPHEN WAYNE 权利人:PFIZER 摘要:Compounds, pharmaceutically acceptable salts thereof, are disclosed wherein the compounds have the structure of (I) as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:AR-116479-A1 优先权日:2018-09-25 标题:INTERMEDIARIES FOR THE SYNTHESIS OF OZANIMOD AND PROCEDURE FOR THE PREPARATION OF THE MENTIONED SPHINGOSINE-1-PHOSPHATE RECEPTOR AGONIST AND SUCH INTERMEDIARIES
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
专利号:US-2023119606-A1 优先权日:2020-02-18 标 题:Immune cell modulators 发明人:SHERDEN NATHANIEL; YU SHEN; STONER ISAAC 权利人:OCTAGON THERAPEUTICS INC 摘要:Disclosed are immune cell-selective small molecule compounds that modulate certain immune cell-specific receptors and enzymes, and methods of their synthesis and use to treat proliferative disorders.