专利号:US-2015105479-A1 优先权日:2012-04-24 标 题:Catalytically active body for the synthesis of dimethyl ether from synthesis gas 发明人:SCHÄFER ALEXANDER; FEYEN MATHIAS; PARVULESCU ANDREI-NICOLAE; Müller Ulrich; SCHAACK BERND BASTIAN 权利人:BASF SE 摘要:The invention relates to a catalytically active body for the synthesis of dimethyl ether from synthesis gas. In particular, the invention relates to an improved catalytically active body for the synthesis of dimethyl ether, whereby the components of the active body comprise a methanol active component and an acid component comprising a zeolitic material being crystallized by means of one or more alkenyltrialkylammonium cation R 1 R 2 R 3 R 4 N + -containing compounds as structure directing agent. Furthermore, the present invention concerns a method for the preparation of a catalytically active body, the use of the catalytically active body and a method for the preparation of dimethyl ether from synthesis gas.
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-6376649-B1 优先权日:1998-12-18 标题 :Methods for the synthesis of α- hydroxy-β-amino acid and amide derivatives 发明人:SEMPLE JOSEPH E; LEVY ODILE E 权利人:CORVAS INT INC 摘要:Methods for the synthesis of alpha-hydroxy-beta-amino acid and amide derivatives and alpha-ketoamide derivatives and novel derivatives made by these methods are provided. These methods involve reacting a N-terminally blocked (protected) aminoaldehyde with an isonitrile and a carboxylic acid to give an amino-alpha-acyloxy carboxamide. The acyloxy group may be removed to give the derivative. Alternatively the protecting group is removed and acyl shift occurs to give the derivative. These derivatives are useful in the synthesis of compounds such as peptidyl alpha-ketoamides and alpha-hydroxy-beta-carboxylic acid and amide derivatives. Certain of these compounds have been reported to have activity as inhibitors of proteases, such as serine proteases and cysteine proteases.
专利号:US-2025101006-A1 优先权日:2022-01-31 标题:Process for the synthesis of pyrazolyl derivatives useful as anti-cancer agents 发明人:BAENZIGER MARKUS; GALLOU FABRICE; GUO FENGFENG; HÄNGGI RUDOLF; HAN ENJIAN; JORDINE GUIDO; LI JIALIANG; LIU WEIPENG; MIAO BUKEYAN; RONG SHAOFENG; SANTANDREA ERNESTO; SCHIRNER PAUL BERND; SHEN XIAODONG; WANG CAN; ZHANG HAO 权利人:NOVARTIS AG 摘要:The invention provides a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, especially KRAS G12C inhibitors. The present invention provides a direct enantioselective chemical manufacturing method of making Compound A, or a pharmaceutically acceptable hydrate or solvent thereof: (I). The invention provides a process for preparing Intermediate B6* comprising reacting Intermediate B4* with Intermediate B5* in an atroposelective coupling reaction, using a chiral catalyst.
专利号:US-4396542-A 优先权日:1980-02-14 标 题 :Method for the total synthesis of cyclosporins, novel cyclosporins and novel intermediates and methods for their production 发明人:WENGER ROLAND 权利人:SANDOZ LTD 摘要:A method for the total synthesis of cyclosporins, in particular Cyclosporin A, cyclosporins produced in accordance with the method of the invention and novel intermediates, in particular novel [1S, 2R, 3R]- and [1R, 2S, 3S]-1-nitrilo-1-carbonyl-3-methyl-2-oxy-heptanes and -hept-5-enes, employed in the method of the invention.
专利号:US-6933385-B2 优先权日:2001-08-03 标题 :Protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use 发明人:WESTERMANN JURGEN; PLATZEK JOHANNES; PETROV ORLIN 权利人:SCHERING AG 摘要:The invention relates to new protected 3,5-dihydroxy-2,2-dimethyl-valeroamides for the synthesis of epothilones and derivatives and process for the production and the use of the new compounds for the production of epothilones or epothilone derivatives.
参考文献:10.1021/acs.jmedchem.2c01438 摘要:Lorthiois E, Gerspacher M, Beyer KS, Vaupel A, Leblanc C, Stringer R, Weiss A, Wilcken R, Guthy DA, Lingel A, Bomio-Confaglia C, Machauer R, Rigollier P, Ottl J, Arz D, Bernet P, Desjonqueres G, Dussauge S, Kazic-Legueux M, Lozac'h MA, Mura C, Sorge M, Todorov M, Warin N, Zink F, Voshol H, Zecri FJ, Sedrani RC, Ostermann N, Brachmann SM, Cotesta S. JDQ443, a Structurally Novel, Pyrazole-Based, Covalent Inhibitor of KRASG12C for the Treatment of Solid Tumors. J Med Chem. 2022 Dec 22;65(24):16173–203. doi: 10.1021/acs.jmedchem.2c01438. 参考文献:10.1016/j.ejmech.2023.115124 摘要:Wang H, Chi L, Yu F, Dai H, Gao C, Si X, Wang Z, Liu L, Zheng J, Shan L, Liu H, Zhang Q. Annual review of KRAS inhibitors in 2022. European Journal of Medicinal Chemistry. 2023 Mar;249():115124. doi: 10.1016/j.ejmech.2023.115124. 参考文献:10.1016/j.ejmech.2023.115698 摘要:Zhao D, Liu Y, Yi F, Zhao X, Lu K. Recent advances in the development of inhibitors targeting KRAS-G12C and its related pathways. European Journal of Medicinal Chemistry. 2023 Nov;259():115698. doi: 10.1016/j.ejmech.2023.115698.