专利号:WO-2025078335-A1 优先权日:2023-10-09 标 题 :Processes for the preparation of deucravacitinib 发明人:ETAYO PÉREZ PABLO; PUJOL OLLÉ XAVIER; MOLINA NIETO JUAN 权利人:FARMHISPANIA GROUP S L 摘要:The invention relates to processes for the preparation of deucravacitinib of formula (XI), or a pharmaceutically acceptable salt thereof. It also relates to intermediates of formula (V') and (V'') as defined herein useful in the synthesis of this molecule.
专利号:US-2009198084-A1 优先权日:2006-05-02 标题:Process for the deprotection of protected amines 发明人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 权利人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 摘要:The present invention relates to a process for the deprotection of protected amine compounds, wherein the protected amine compound is contacted with an electrophilic oxidating agent that is optionally formed in situ, said electrophilic oxidating agent being selected from the group of I 2 , Br 2 , Cl 2 and compounds comprising a halogen atom having a formal oxidation state of 1+, 3+, 5+ or 7+, provided that the electrophilic oxidating agent is not iodobenzene diacetate. The process can be conveniently employed in the synthesis of 1,3-amino alcohols, β-amino acids and heterocyclic compounds, in particular β-amino acids.
专利号:US-6096900-A 优先权日:1999-05-07 标 题 :Solventless preparation of phthalimides 发明人:NICK ROBERT JOSEPH; NELSON MARK ERIK; CARINGI JOSEPH JOHN; WILLIAMS DREW ELLIOT 权利人:GEN ELECTRIC 摘要:A method for the solventless synthesis of a phthalimide or phthalimide mixture is provided comprising contacting at least one amine reactant and at least one anhydride reactant in a solventless environment at a first temperature sufficient to allow the reactants to at least partially condense; and increasing the temperature to a second temperature sufficient to melt the reaction mixture, thereby allowing the reaction to go essentially to completion and form the reaction product.
专利号:WO-0146142-A1 优先权日:1999-12-20 标题:A process for the regioselective synthesis of 2,2-dialkyl-4-substituted piperidines 发明人:HEATH PERRY CLARK 权利人:LILLY CO ELI; HEATH PERRY CLARK 摘要:The present invention provides a process for preparing a compound of formula (I): wherein R?1 and R2¿ each independently represent C¿1?-C4 alkyl; and X represents an alkyl, alkenyl, cycloalkyl, aryl, substituted aryl, heterocycle, or substituted heterocycle, comprising treating a compound of formula (II): wherein Q represents Cl or Br, with a suitable base followed by addition of a suitable Lewis acid and addition of a compound of formula R?-M+¿ wherein M+ is a suitable cation.
专利号:US-2022056025-A1 优先权日:2018-09-25 标 题:Synthesis of pyrido[2,3-d]pyrimidin-7(8h)-ones 发明人:BROWN ADAM ROSS; DESROSIERS JEAN-NICOLAS; DUAN SHENGQUAN; HAWKINS JOEL MICHAEL; HAYWARD CHERYL MYERS; MALONEY MARK THOMAS; MONFETTE SEBASTIEN; PERFECT HAHDI HAKIMIOUN; WIDLICKA DANIEL WILLIAM 权利人:PFIZER 摘要:This invention relates to novel methods to prepare substituted pyrido[2,3-d]pyrimidin-7(8H)-ones, and salts and stereoisomers thereof, as well as intermediates useful for the preparation of such compounds.
专利号:US-2022056053-A1 优先权日:2019-05-06 标 题:Synthesis of crac channel inhibitors 发明人:STAUDERMAN KENNETH A; DUNN MICHAEL; WHITTEN JEFFREY P; ROGERS EVAN 权利人:CALCIMEDICA INC 摘要:A convergent synthetic method for the production of CRAC channel inhibitors is described herein. The synthetic method provides a method for producing highly pure CRAC channel inhibitors for clinical testing.