专利号:US-2024308959-A1 优先权日:2021-06-29 标 题:Processes for the preparation of (s)-2-(4-chloro-2-methoxyphenyl)-2-((3 -methoxy-5-(m ethylsulfonyl)phenyl)amino)-1 -(1h-indol-3-yl)ethenone derivatives 发明人:WU KAI; OOST RIK; SCHWEITZER-CHAPUT BERTRAND; ERIKSSON CARL ARNE MAGNUS; COESEMANS ERWIN 权利人:JANSSEN PHARMACEUTICALS INC 摘要:The present invention relates to novel chiral synthesis of mono- or di-substituted indole compounds of formula (I) n n n n n n n n n n n n wherein: n R 1 is H, R 2 is F and R 3 is H or CH 3 , n R 1 is H, CH 3 or F, R 2 is OCH 3 and R 3 is H and n R 1 is H, R 2 is OCH 3 and R 3 is CH 3 , n R 1 is CH 3 , R 2 is F and R 3 is H, n R 1 is CF 3 or OCF 3 , R 2 is H and R 3 is H, n R 1 is OCF 3 , R 2 is OCH 3 and R 3 is H and n R 1 is OCF 3 , R 2 is H and R 3 is CH 3 .
专利号:US-2004110228-A1 优先权日:2002-04-01 标 题:Combinatorial organic synthesis of unique biologically active compounds 发明人:MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M 摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.
专利号:US-11566004-B2 优先权日:2018-07-23 标题 :Process for the preparation of bromodomain inhibitor 发明人:TRAVERSE JOHN FITZGERALD; YONG KELVIN HIN-YEONG; FERRETTI ANTONIO CHRISTIAN; ALITE HEKLA; MOSELEY JONATHAN; RUDA ANTONIO MARIA; PRIMER DAVID; PHILP STEVEN 权利人:CELGENE QUANTICEL RES INC 摘要:The present invention provides processes of synthesis and purification of a bromodomain inhibitor, Compound 1, which compound includes crystalline forms, amorphous forms, solvates, and hydrates thereof. Embodiments of the disclosure relate to chemical synthesis routes of Compound 1 that provide a scalable method that results in highly pure final product. A further embodiment relates to methods to isolate the most stable polymorph of Compound 1 by crystallization from formic acid and water.
专利号:WO-2025198684-A2 优先权日:2023-12-20 标题 :BaTiO3 NANOCRYSTALS AND NANOCOMPOSITES 发明人:SZYCHOWSKI BRIAN; GELLEN TOBIAS A; WIACEK ROBERT J; MONICKAM SELINA THOMAS; WILLIAMS ZEHRA SERPIL GONEN; FU GUOYI 权利人:PIXELLIGENT TECH LLC 摘要:The synthesis of barium titanate nanocrystals, the capping of barium titanate nanocrystals to disperse into solvents, including polar and nonpolar solvents, polyalphaolefins, lubricants, oils, and greases, monomers, oligomers, and polymers including acrylics, epoxies, siloxanes, and the preparation of nanocomposites of barium titanate in combination with these monomers, oligomers, and polymers. The barium titanate nanocrystals are monodispersed with sizes between 1-200 nm and have an ideal barium to titanium ratio. The nanocrystals of size greater than 80 nanometer can possess high dielectric constants and can be ideal candidates of ceramic conductors and RF sensors. Nanocomposites resulting from the barium titanate nanocrystals of size less than 40 nanometer in combination with the monomers, oligomers, and polymers can possess high refractive index, high transparency, low absorbance, and minimal change when exposed to heat or UV light.
专利号:US-9321713-B2 优先权日:2011-06-03 标 题:Hyperforin analogs, methods of synthesis, and uses thereof 发明人:SHAIR MATTHEW D; SPARLING BRIAN A; MOEBIUS DAVID 权利人:SHAIR MATTHEW D; SPARLING BRIAN A; MOEBIUS DAVID; HARVARD COLLEGE 摘要:The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisioned useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.
专利号:TW-201040144-A 优先权日:2009-03-31 标 题:New process for the synthesis of ivabradine and addition salts thereof with a pharmaceutically acceptable acid
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合成参考文献
摘要:Il'chenko, A. Y., Science of Synthesis, (2005) 18, 1169.