📜1,1'-氧基二(环己烷)置于磷化氢,氢碘酸体系中,化学反应生成 碘环己烷 参考文献:Lacourt,Bulletin Des Societes Chimiques Belges,1927,Vol. 36,P. 348,350,352 标题:Lacourt,Bulletin Des Societes Chimiques Belges,1927,Vol. 36,P. 348,350,352
专利信息
专利号:US-9802953-B2 优先权日:2007-10-03 标 题 :Intermediates and methods for the synthesis of halichondrin B analogs 发明人:CHASE CHARLES E; ENDO ATSUSHI; FANG FRANCIS G; LI JING 权利人:EISAI R&D MAN CO LTD 摘要:Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
专利号:WO-2017082924-A1 优先权日:2015-11-13 标题 :Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE TERRENCE R JR; HYMEL DAVID 权利人:THE US SECRETARY DEPT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
专利号:WO-2014128524-A1 优先权日:2013-02-19 标题:An improved process for preparation of an intermediate of the pyrrolidine substituted flavones 发明人:CHENNAMSETTY SUNEELMANOHARBABU; PATIL RAJENDRA; HAREL PRASHANT; HARIHARAN SIVARAMAKRISHNAN 权利人:PIRAMAL ENTPR LTD 摘要:The present invention relates to a process for the preparation of a key intermediate (as described herein) used in the synthesis of (+)- trans enantiomer of pyrrolidine substituted flavones, represented by the compounds of formula (1) or pharmaceutically acceptable salts thereof; which are inhibitors of cyclin dependant kinases (CDKs) and can be used in the treatment of proliferative disorders such as cancer. Formula (1) wherein R 1 has the meaning as indicated in the claims. The process of the present invention has advantages of higher yield and purity, lower reaction temperature, is consistent and involves the use of non toxic solvents. The process of the present invention allows efficient large-scale synthesis and purity of the product obtained is greater than 97 %.
专利号:WO-2014128523-A1 优先权日:2013-02-19 标 题 :A process for preparation of an intermediate of the pyrrolidine substituted flavones 发明人:CHENNAMSETTY SUNEELMANOHARBABU; BOKKA RAVISHANKAR; VEERAPPAN RATHINASAMI; SIVAKUMAR MEENAKSHI; HARIHARAN SIVARAMAKRISHNAN 权利人:PIRAMAL ENTPR LTD 摘要:The present invention relates to a process for the preparation of a key intermediate (as described herein) used in the synthesis of (+)- trans enantiomer of pyrrolidine substituted flavones, represented by the compounds of formula (1) or pharmaceutically acceptable salts thereof; which are inhibitors of cyclin dependant kinases (CDKs) and can be used in the treatment of proliferative disorders such as cancer. Formula (1) wherein R has the meaning as indicated in the claims. The process of the present invention has advantages of higher yield and purity, lower reaction temperature, is consistent and involves the use of non toxic solvents. The process of the present invention allows efficient large-scale synthesis and purity of the product obtained is greater than 97 %.
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-2008183007-A1 优先权日:2004-10-08 标 题 :Process For the Preparation of Alkyl Phosphinic Acids 发明人:THELIN MATS 权利人:ASTRAZENECA AB 摘要:The present invention relates to a new process for the synthesis of alkyl phosphinic acids, and more particularly to a coupling reaction between an alkylhalide and a hypophosphorous acid derivative by a radical initiated reaction. The invention also relates to compounds obtainable by the method of the invention.
[参考文献]: Jun Yi, Et Al. Nickel-Catalyzed Sonogashira Reactions Of Non-Activated Secondary Alkyl Bromides And Iodides. Angew Chem Int Ed Engl. 2013 Nov 18;52(47):12409-13.
合成参考文献
摘要:Li, Y.; Xie, W.; Jiang, X., Science of Synthesis Knowledge Updates, (2016) 2, 27. 摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 51. 摘要:Li, Y.; Xie, W.; Jiang, X., Science of Synthesis Knowledge Updates, (2016) 2, 16. 摘要:Kostikov, R. R.; Khlebnikov, A. F.; Sokolov, V. V., Science of Synthesis, (2010) 47, 780. 摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 32.