专利号:US-2023357286-A1 优先权日:2020-07-24 标 题:Ketone synthesis and applications 发明人:KISHI YOSHITO; UMEHARA ATSUSHI 权利人:HARVARD COLLEGE 摘要:Provided are new nickel./zirconium-mediated coupling reactions useful in the synthesis of ketone-containing compounds, e.g., halichondrin natural products and related molecules. A feature of the present disclosure is the use of a nickel(I) catalyst in tandem with a nickel (II) catalyst in the Ni/Zr-mediated coupling reactions. Without wishing to be bound by any particular theory, the nickel (I) catalyst selectively activates the electrophilic coupling partner (i.e., the compound of Formula (A)), and the nickel(ll) catalyst selectively activates the nucleophilic coupling partner (i.e., a thioester of Formula (B)). This dual catalyst system leads to improved coupling efficiency and eliminates the need for a large excess of one of the coupling partners (i.e., a compound of Formula (A) or (B)).
专利号:US-6642390-B2 优先权日:2001-07-11 标 题:One step synthesis of 1,2,3-triazole carboxylic acids 发明人:KOLB HARTMUTH C; CAVALLARO CULLEN; SHI ZHI-CAI; GONTCHAROV ALEXANDER; WANG ZHI-MIN; RICHARDSON PAUL F; KANAMARLAPUDI RAMANAIAH C 权利人:LEXICON PHARMACEUTICALS INC 摘要:Disclosed is a one step method for preparing a 1,2,3-triazole carboxylic acid by treating an azide with a beta-ketoester in the presence of a base.
专利号:US-2003135050-A1 优先权日:2001-07-11 标题 :One step synthesis of 1,2,3-triazole carboxylic acids
专利号:US-2012295923-A1 优先权日:2010-01-29 标 题:Aminocyclohexanes and Aminotetrahydropyrans and Related Compounds As Gamma-Secretase Modulators 发明人:AM ENDE CHRISTOPHER WILLIAM; FISH BENJAMIN ADAM; JOHNSON DOUGLAS SCOTT; LIRA RICARDO; O'DONNELL CHRISTOPHER JOHN; PETTERSSON MARTIN YOUNGJIN; STIFF COREY MICHAEL 权利人:AM ENDE CHRISTOPHER WILLIAM; FISH BENJAMIN ADAM; JOHNSON DOUGLAS SCOTT; LIRA RICARDO; O'DONNELL CHRISTOPHER JOHN; PETTERSSON MARTIN YOUNGJIN; STIFF COREY MICHAEL; PFIZER 摘要:Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I n n n n n n n n n n as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
专利号:WO-2022012456-A1 优先权日:2020-07-17 标题:Novel heterocyclic compounds as bet inhibitors 发明人:FANG HAIQUAN; LUO XINFENG; SHU TIANBO; ZHANG JIBING; WU XIANQIANG; ZHU HUI; WANG YING 权利人:CHENGDU EASTON BIOPHARMACEUTICALS CO LTD 摘要:Provided are heterocyclic compounds of formula (I) as bromodomain and extraterminal (BET) inhibitors, pharmaceutical compositions comprising the compounds, their synthesis and their use for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.
专利号:US-6613942-B1 优先权日:1997-07-01 标题 :Glucagon antagonists/inverse agonists 发明人:LING ANTHONY; GREGOR VLAD; GONZALEZ JAVIER; HONG YUFENG; KIEL DAN; KUKI ATSUO; SHI SHENGHUA; NAERUM LARS; MADSEN PETER; SAMS CHRISTIAN; LAU JESPER; PLEWE MICHAEL BRUNO; FENG JUN; TENG MIN; JOHNSON MICHAEL DAVID; TESTON KIMBERLY ANN; SIDELMANN ULLA GROVE; KNUDSEN LOTTE BJERRE 权利人:NOVO NORDISK AS 摘要:Non-peptide compounds comprising a central hydrazide motif and methods for the synthesis thereof are disclosed. The compounds act to antagonize the action of the glucagon peptide hormone.
[参考文献]: Gary A Molander, Et Al. Nickel-Catalyzed Cross-Coupling Of Potassium Aryl- And Heteroaryltrifluoroborates With Unactivated Alkyl Halides. Org Lett. 2010 Dec 17;12(24):5783-5.
合成参考文献
摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 193. 摘要:Littke, A., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 1, 258.