专利号:US-9353057-B2 优先权日:2003-12-30 标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof 发明人:GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA 权利人:XENOPORT INC 摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.
专利号:US-2012177593-A1 优先权日:2009-07-20 标 题 :Synthesis of dendrimer conjugates 发明人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH 权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN 摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.
专利号:WO-2023019298-A1 优先权日:2021-08-20 标 题:Improved method of synthesis of 1-(3',4'-methylene dioxyphenyl)-2-(methylamino) propane (mdma) 发明人:O'MALLEY WILLIAM IAN; WYNNE PAUL MICHAEL 权利人:MIND MEDICINE AUSTRALIA LTD 摘要:The present invention relates to an improved method of synthesis of 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA) that is of sufficient purity that it can be used for pharmaceutical applications. In particular the present invention provides a method of synthesising MDMA comprising the steps of (a) condensation of piperonal and nitroethane in the presence of a catalysing base to form 1-(3',4'-methylenedioxyphenyl)-2-nitroprop-1-ene (MDP-2-nitropropene), (b) oxidative hydrolysis of MDP-2-nitropropene to form 1-(3',4'methylenedioxyphenyl)-propan-2-one (MDP2P), and (c) reductive amination of MDP2P to 1-(3',4'-methylenedioxyphenyl)-2-(methylamino)propane (MDMA).
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-10266481-B2 优先权日:2014-06-20 标题:Organocatalytic asymmetric synthesis of antidepressants 发明人:VAITHIYANATHAN VENKATARAMASUBRAMANIAN; KALSHETTI RUPALI GUNDAPPA; ARUMUGAM SUDALAI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention relates to a short enantioselective synthesis of 1-amino aryl tetraline compounds of Formula 1 via nucleophilic enamine catalysis using organocatalyst such as proline. n n n n n n n n n n n n wherein R 1 and R 2 represent independent of each other hydrogen, (un)substituted or substituted amine; n R 3 and R 4 represent independent of each other hydrogen or halogen.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
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