专利号:US-9139515-B2 优先权日:2011-08-19 标 题:Synthesis of R-biphenylalaninol 发明人:HERMSEN PETRUS JOHANNES; ERMANN PETER HANS; RIEBEL PETER HANS; WOLBERG MICHAEL; DE VRIES ANDREAS HENDRIKUS MARIA 权利人:HERMSEN PETRUS JOHANNES; ERMANN PETER HANS; RIEBEL PETER HANS; WOLBERG MICHAEL; DE VRIES ANDREAS HENDRIKUS MARIA; DPX HOLDINGS BV 摘要:This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
专利号:US-10040752-B2 优先权日:2015-08-24 标 题 :Synthesis of levomethadone hydrochloride or dextromethadone hydrochloride and methods for use thereof 发明人:MKRTCHYAN GNEL; YAO QINGWEI 权利人:CODY LABORATORIES INC 摘要:Highly efficient methods for synthesis of levomethadone hydrochloride or dextromethadone hydrochloride are provided starting from D-alanine, or L-alanine, respectively, with retention of configuration. Methods for treating a subject are provided comprising administering a composition comprising an effective amount of levomethadone hydrochloride having not more than 10 ppm dextromethadone.
专利号:US-5869725-A 优先权日:1994-05-17 标 题:Derivatives of aminosulfonic acids, utilization of the same in the synthesis of pseudopeptides and process for their preparation 发明人:GENNARI CESARE; POTENZA DONATELLA; SALOM BARBARA 权利人:PHARMACIA & UPJOHN SPA 摘要:Derivatives of gamma-amino-alpha,beta-unsaturated sulfonic acids, a process for the preparation of the same and their utilization in the synthesis of pseudopeptides characterized by the presence of at least a sulfonamide type bond conjugated to a double bond are described.
专利号:US-2006058532-A1 优先权日:2004-09-10 标 题:Process for the scalable synthesis of 1,3,4,9-tetrahydropyrano[3,4-b]-indole derivatives 发明人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 权利人:CHEW WARREN; CHEAL GLORIA K; LUNETTA JACQUELINE F; DEMERSON CHRISTOPHER A 摘要:The invention is directed to a process of synthesizing compounds of formula (VI): n n nwherein R 1- R 9 , R 3′ , R 4′ and Y are as set forth in the specification, and said method is useful for large scale synthesis thereof. The invention is also directed to useful intermediates for synthesizing the compounds of formula (VI) and processes of preparing said intermediates.
专利号:US-8440844-B2 优先权日:2011-06-21 标题 :Process for the preparation of β-amino alcohol 发明人:RAWAT VARUN; CHOUTHAIWALE PANDURANG VILASRAO; CHAVAN VILAS BHIKU; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM 权利人:RAWAT VARUN; CHOUTHAIWALE PANDURANG VILASRAO; CHAVAN VILAS BHIKU; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM; COUNCIL SCIENT IND RES 摘要:A high-yielding enantioselective synthesis of the bioactive (S)—N-(5-chlorothiophene-2-sulfonyl)-β,β-diethylalaniol (7.b.2), a Notch-1-sparing γ-secretase inhibitor metabolite (with EC 50 =28 nM) effective in reduction of Aβ production in vivo, has been realized starting from readily available 3-pentanone. The key steps of the synthesis are proline-catalyzed α-aminooxylation and α-amination of aldehyde; the latter contributing an overall yield of 50-75% and 90-99% enantiomeric excess.
专利号:US-11717498-B2 优先权日:2013-12-31 标题 :Methods of treatment using amphetamine controlled release, prodrug, and abuse deterrent dosage forms 发明人:POPP KARL; MECKLER HAROLD 权利人:Chemapotheca LLC; PHARMAPOTHECA A INC 摘要:The invention also relates to pharmaceutical compositions comprising highly pure amphetamine and amphetamine-class compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds, and to methods of manufacturing, delivering, and using the amphetamine compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds.
摘要:Schoonen, L.; te Grotenhuis, C.; Rutjes, F. P. J. T., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 249. 摘要:Bertau, M.; Jeromin, G. E., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 161. 摘要:Besson, M.; Pinel, C., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 278. 摘要:Kayaki, Y.; Ikariya, T., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 98. 摘要:Shi, Y.; Cole-Hamilton, D. J.; Kamer, P. C. J., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2017) 2, 200.