专利号:US-9643915-B2 优先权日:2013-03-15 标题:Methods for the synthesis of sphingomyelins and dihydrosphingomyelins 发明人:ONICIU DANIELA CARMEN; HECKHOFF STEFAN; OSWALD BENOIT; REBMANN PETER; PEER ANDREAS; GONZALEZ MIGUEL; SAUTER PATRIK 权利人:CERENIS THERAPEUTICS HOLDING SA 摘要:The present invention includes methods for the synthesis of sphingomyelins and dihydrosphingomyelins. The present invention also includes methods for the synthesis of sphingosines and dihydrosphingosines. The present invention further includes methods for the synthesis of ceramides and dihydroceramides.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.
专利号:US-9428482-B2 优先权日:2011-01-27 标 题 :Process for synthesis of polyphenols 发明人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE 权利人:DUGAR SUNDEEP; MAHAJAN DINESH; PANTELIS PETER GIANNOUSIS; SINGH VIJAY; KAPOOR KAMAL KISHORE; SPHAERA PHARMA PTE LTD 摘要:The present invention provides synthetic processes for preparing racemic and/or optically pure epicatechin, epigallocatechin and related polyphenols as such or as their variously functionalized derivatives. A principle objective of the disclosure is to provide a new and useful method of synthesis to obtain polyphenols in isomerically pure and/or racemic forms.
专利号:US-6469193-B1 优先权日:1999-02-26 标 题 :Efficient synthesis of alkyl carbonates 发明人:JUNG KYUNG WOON 权利人:UNIV SOUTH FLORIDA 摘要:Efficient synthetic methods towards mixed aliphatic carbonates through the three component couplings of aliphatic alcohols, alkyl halides and carbon dioxide in the presence of cesium carbonate and tetrabutylammonium iode (TBAI). Due to their enhanced nucleophilicities, cesium alkoxides are smoothly incorporated into CO 2 , allowing for mild reaction conditions such as ambient temperatures and short reaction durations. Various primary and secondary substrates are compatible under the standard conditions, offering high yields, while chiral templates such as α-hydroxy carbonyls are resistant to racemization.
专利号:US-8981121-B2 优先权日:2010-06-25 标 题 :Process for the preparation of nitrogen substituted aminotetralins derivatives 发明人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE 权利人:ATES CELAL; SCHULE ARNAUD; PALACIO MAGALI; DEUTSCH PAUL; VASSELIN DAVID; CARLY NICOLAS; PHADTARE GANESH; YERANDE SWAPNIL; DELATINNE JEAN-PIERRE; ESCUDERO HERNANDEZ MARIA LUISA; PINILLA VERONIQUE; UCB PHARMA GMBH 摘要:The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R 1 , R 2 and R 3 are as defined for compound of formula (I).
专利号:US-10030003-B2 优先权日:2014-09-10 标 题:Synthesis of isoflavanes and intermediates thereof 发明人:BELIAEV NIKOLAI; SHAFRAN YURI 权利人:SYSTEM BIOLOGIE AG 摘要:Subject of the invention is a method for enantioselective production of an isoflavane from an isoflavone, comprising the steps: (a) selectively reducing the isoflavone, such that the 4-keto group of the isoflavone is converted to a 4-hydroxy group, and the 2,3-double bond of the isoflavone is converted to a 2,3-single bond, thereby obtaining a 4-hydroxy intermediate, and (b) reacting the 4-hydroxy intermediate with a chiral reagent, such that a chiral group is covalently attached to the C4-position of the 4-hydroxy intermediate, thereby obtaining a chiral intermediate. The invention also relates to intermediates of formulae (IV), (V), (VI) and (VII) obtainable in the inventive process.
[参考文献]: Radoslaw Laufer, Et Al. Discovery Of Inhibitors Of The Mitotic Kinase Ttk Based On N-(3-(3-Sulfamoylphenyl)-1H-Indazol-5-Yl)-Acetamides And Carboxamides. Bioorg Med Chem. 2014 Sep 1;22(17):4968-97.
合成参考文献
摘要:Stoltz, B. M.; Mohr, J. T., Science of Synthesis: Stereoselective Synthesis, (2011) 3, 620. 摘要:Leclerc, E., Science of Synthesis: Knowledge Updates, (2024) 3, 241. 摘要:Sawamura, M.; Shimizu, Y., Science of Synthesis: Knowledge Updates, (2024) 2, 223.