专利号:WO-2025215126-A1 优先权日:2024-04-12 标题:Synthesis of vidofludimus and its calcium salt 发明人:VITT DANIEL; IGLICAR PETRA; GEGE CHRISTIAN; Mühler Andreas; KOHLHOF HELLA; GRÖPPEL MANFRED 权利人:IMMUNIC AG 摘要:The invention relates to the process of preparation of 2-fluoro-4-(3-methoxyphenyl)aniline (3) as an intermediate. Said intermediate 2-fluoro-4-(3-methoxyphenyl)aniline (3) is obtained in a Suzuki coupling reaction from (3-methoxyphenyl)boronic acid (1) and 4-bromo-2-fluoro-aniline (2). The invention further relates to the synthesis of vidofludimus (5) from said intermediate 2-fluoro-4-(3-methoxy-phenyl)aniline (3) and from 1-cyclopentene-1,2-dicarboxylic anhydride (4). The invention further relates to the synthesis of vidofludimus calcium (6) from said vidofludimus (5) and from a calcium salt, preferably Ca(OH)2.
专利号:US-6262272-B1 优先权日:1997-11-13 标题 :Method of synthesis of pyrrole amides 发明人:RAGAN JOHN ANTHONY; MAKOWSKI TERESA WOODALL; AM ENDE DAVID JON; CLIFFORD PAMELA JANE; YOUNG GREGORY RANDALL; CONRAD ALYSON KAY; EISENBEIS SHANE ALLEN; QUALLICH GEORGE JOSEPH; ALLEN DOUGLAS JOHN MELDRUM 权利人:PFIZER 摘要:A method for preparing pyrrole-carboxyamides which selectively bind to GABAa receptors; which comprises reacting 1,3-cycloakane-diones with bromoethylacetate followed by reaction of the resulting product with an acid halide followed by reaction with an aromatic amine and finally with an amonium source at an elevated temperature.
专利号:US-6465656-B2 优先权日:1999-10-21 标题 :Synthesis of 1,3,5-trisubstituted pyrazoles 发明人:ZHOU JIACHENG; OH LYNETTE MAY; CONFALONE PASQUALE N; LI HUI-YIN; MA PHILIP 权利人:BRISTOL MYERS SQUIBB PHARMA CO 摘要:A novel process for making 1,3,5-trisubstituted pyrazoles of the type shown below from appropriate phenyl hydrazines is described. n These compounds are useful as factor Xa inhibitors.
专利号:US-6531470-B1 优先权日:1998-01-23 标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation 发明人:GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC 权利人:UPJOHN CO 摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
专利号:US-6329527-B1 优先权日:1999-10-21 标题 :Synthesis of 1,3,5-trisubstituted pyrazoles
专利号:WO-9925684-A1 优先权日:1997-11-13 标题 :Method of synthesis of pyrrole amides
[参考文献]: Catherine J Duckett, Et Al. High-Performance Liquid Chromatography/inductively Coupled Plasma Mass Spectrometry With Iodine-Specific Detection For Profiling The Metabolites Produced In The Earthworm Eisenia Veneta By Exposure To 2-Fluoro-4-Iodoaniline. Rapid Commun Mass Spectrom. 2003;17(16):1855-8.
合成参考文献
摘要:Tomé, A. C., Science of Synthesis Knowledge Updates, (2015) 2, 99. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 80. 摘要:Maestri, G.; Serafino, A., Science of Synthesis, (2021) , 658. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2026).