专利号:US-2012029226-A1 优先权日:2009-02-06 标题:Method for the synthesis of chiral alpha-aryl propionic acid derivatives 发明人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 权利人:KAPTEIN BERNARDUS; VLIEG ELIAS; NOORDUIN WILLEM LIEUWE 摘要:The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as grinding.
专利号:EP-2589587-A1 优先权日:2011-11-04 标题:Synthesis of nitrogen substituted cyclopropanes 发明人:RASPARINI MARCELLO; TADDEI MAURIZIO; CINI ELENA; MINELLI COSIMA; TURNER NICHOLAS; HUGENTOBLER KATHARINA GLORIA 权利人:CHEMO IBERICA SA 摘要:The invention is about a new synthetic pathway for the preparation of enantiomerically pure nitrogen substituted cyclopropanes, in particular the trans- cyclopropanamine ( 1 ), a key intermediate in the synthesis of Ticagrelor:n n The invention also relates to the processes for preparing said compounds or their salts and the use of said compounds as intermediates in preparing pharmaceutically active ingredients.
专利号:US-8420850-B2 优先权日:2010-05-14 标 题:Compounds for the synthesis of biostable polyurethane, polyurea or polyurea urethane polymers 发明人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE 权利人:DUOCASTELLA CODINA LLUIS; MOLINA MARIA; ARAD OFIR; BORRELL BILBAO JOSE IGNACIO; GARCIA DAVID SANCHEZ; PETTERSON SALOM SOFIA HENRIETTE; IBERHOSPITEX SA 摘要:The invention comprises compounds which are derived from a drug or a substance with therapeutic properties, and useful as reagents for the synthesis of biostable polymers including said drug in their backbone, namely polyurethanes, polyureas or polyurea urethanes that are biocompatible and biostable. The invention also comprises the processes for preparing the compounds and the polymers, and to the use of these polymers for the manufacture of medical devices.
专利号:US-8304409-B2 优先权日:2002-07-03 标 题:Nitrosated nonsteroidal antiinflammatory compounds, compositions and methods of use 发明人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI 权利人:EARL RICHARD A; EZAWA MAIKO; FANG XINQIN; GARVEY DAVID S; GASTON RICKY D; KHANAPURE SUBHASH P; LETTS L GORDON; LIN CHIA-EN; RANATUNGE RAMANI R; RICHARDSON STEWART K; SCHROEDER JOSEPH D; STEVENSON CHERI A; WEY SHIOW-JYI; NICOX SA 摘要:The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides methods for treating inflammation, pain and fever; for treating gastrointestinal disorders; for facilitating wound healing; for treating and/or preventing gastrointestinal, renal and/or respiratory toxicities resulting from the use of nonsteroidal antiinflammatory compounds; for treating inflammatory disease states and/or disorders; and for treating and/or preventing ophthalmic diseases and/or disorders.
专利号:US-5750764-A 优先权日:1995-11-17 标题 :Synthesis and resolution of propionic acid derivatives 发明人:MARAIS STEPHANUS FRANCOIS; KHAILE THEBEEAPELO JOHN; NJAMELA OWEN LUNGILE; BRAITHWAITE DANA HELEN; DAVIDSON DEBORAH NICOLE; JUNGMANN CHRISTA MARIA; PARKINSON CHRISTOPHER JOHN; GARDINER NEIL STOCKENSTROM; STEENKAMP LUCIA HENDRINA; VAN EEDEN SKEIN ETIENNE 权利人:AECI LTD 摘要:A process for the production of disubstituted propionic acid derivatives which are intermediates in the synthesis of α-arylpropionic acids such as naproxen, involves the reaction of a naphthalene derivative such as 2-methoxynaphthalene, with an alkylating agent such as an alkyl pyruvate in the presence of a catalyst, and then dehydrating and hydrogenolising, or directly hydrogenolising, or derivatising and then hydrogenolising the product thereof, to produce the desired compound.
专利号:US-5023381-A 优先权日:1988-12-22 标 题 :Process for preparing an organic synthesis intermediate 发明人:PERDONCIN GIULIO; GIORDANO CLAUDIO; PAIOCCHI MAURIZIO; CASAGRANDE ROBERTO 权利人:ZAMBON SPA 摘要:A process is described for the preparation of 2-methoxy-6-propionyl-naphthalene, an intermediate in the synthesis of naproxen. n The process consists of Friedel-Crafts acylation of 2-methoxy-naphthalene, and obviates the drawbacks related to the use of nitrobenzene as solvent.
1: Wang W, Gong J, Zhao J, Zhang H, Wen W, Zhao Z, Li YJ, Wang J, Huang CZ, Gao PF. Integration of Wallach's Rule into Intermolecular Charge Transfer: A Visual Strategy for Chiral Purification. Adv Sci (Weinh). 2024 Jul 16:e2403249. doi: 10.1002/advs.202403249. Epub ahead of print. 146(21):14433-14438. doi: 10.1021/jacs.4c04164. Epub 2024 May 17. 96(14):5580-5588. doi: 10.1021/acs.analchem.4c00040. Epub 2024 Mar 26. 89(8):e202400021. doi: 10.1002/cplu.202400021. Epub 2024 Mar 22. 35(9):636-644. doi: 10.1002/chir.23564. Epub 2023 Mar 23. 35(5):311-322. doi: 10.1002/chir.23541. Epub 2023 Feb 7. 1687:463684. doi: 10.1016/j.chroma.2022.463684. Epub 2022 Nov 26. 33(12):938-950. doi: 10.1002/chir.23369. Epub 2021 Oct 15. 29(5):1261-1278. doi: 10.1007/s10787-021-00871-2. Epub 2021 Sep 12. 13(8):1253. doi: 10.3390/pharmaceutics13081253.
合成参考文献
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