专利号:US-11161827-B2 优先权日:2019-04-05 标 题 :Catalytic systems for stereoselective synthesis of chiral amines by enantiodivergent radical C—H amination 发明人:Zhang xiao-xiang; Lang kai 权利人:TRUSTEES BOSTON COLLEGE; THE TRUSTEES OF BOSTON COLLEGE 摘要:In one aspect, the disclosure relates to a mode of asymmetric induction in radical processes based on sequential combination of enantiodifferentiative H-atom abstraction and stereoretentive radical substitution. Also disclosed is an asymmetric system for stereoselective synthesis of strained 5-membered cyclic sulfamides via radical 1,5-C—H amination of sulfamoyl azides. The disclosed metalloradical system can control the degree and sense of asymmetric induction in the catalytic radical C—H amination in a systematic manner. The disclosed system is applicable to a broad scope of substrates with different types of C(sp 3 )—H bonds and exhibits reactivity and selectivity, providing access to both enantiomers of useful 5-membered cyclic sulfamides in a highly enantioenriched form. Also disclosed are catalysts useful in these processes. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present disclosure.
专利号:US-8759555-B2 优先权日:2004-03-18 标 题:Stereoselective synthesis of vitamin D analogues 发明人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN 权利人:SABROE THOMAS PETER; CALVERLEY MARTIN JOHN; LEO PHARMA AS 摘要:The present invention relates to intermediates useful for the synthesis of calcipotriol or calcipotriol monohydrate, to methods of producing said intermediates, and to methods of stereoselectively reducing said intermediates.
专利号:US-10059653-B2 优先权日:2015-01-20 标 题 :Process for the preparation of indanamine derivatives and new synthesis intermediates 发明人:BERTOLINI GIORGIO; CEREA PAOLANGELO; COLLI CORRADO; FELICIANI LAZZARO; GASSA FEDERICO; BIANCHI ALDO; COLOMBO FEDERICA; MAIORANA STEFANO; NISIC FILIPPO 权利人:LABORATORIO CHIMICO INT S P A; OLON SPA 摘要:Subject-matter of the invention is a process for the preparation of a key intermediate in the synthesis of indacaterol. Subject-matter of the invention are also new synthesis intermediates. Formula (I):
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-7199274-B2 优先权日:2002-10-22 标 题:Preparation of substituted indenes 发明人:SCHULTE JOERG; SCHOTTEK JOERG; FISCH LOTHAR 权利人:BASELL POLYOLEFINE GMBH 摘要:The present invention relates to a simple process for preparing specifically substituted indenes of the formula (I) or (Ia) n nto compounds of the formula (II) serving as starting materialsn n nand to the use of the compounds of the formula (II) as starting materials for the synthesis of substituted indenes.
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.
[参考文献]: Abdulaziz A Al-Saadi, Et Al. Spectroscopic And Computational Studies Of The Intramolecular Hydrogen Bonding Of 2-Indanol. J Phys Chem A. 2006 Nov 9;110(44):12292-7. [参考文献]: Giuliana Donadio, Et Al. The Toluene O-Xylene Monooxygenase Enzymatic Activity For The Biosynthesis Of Aromatic Antioxidants. Plos One. 2015 Apr 27;10(4):E0124427.
合成参考文献
摘要:Li, H.; Wang, Y.; Liu, Q., Science of Synthesis: Base-Metal Catalysis, (2023) 2, 511. 摘要:Arimitsu, S.; Cahard, D., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 28. 摘要:Xu, C.; Shao, X.; Shen, Q., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 59. 摘要:Bertrand, X.; Paquin, J.-F., Science of Synthesis: Modern Strategies in Organofluorine Chemistry, (2025) 2. 参考文献:10.1063/1.2201747 摘要:He Y, Kong W. Resonantly enhanced multiphoton ionization and zero kinetic energy photoelectron spectroscopy of 2-indanol conformers. J Chem Phys. 2006 May 28;124(20):204306. doi: 10.1063/1.2201747.