专利号:US-8314246-B2 优先权日:2005-08-30 标题:Catalytic reactions involving alkenes 发明人:JAMISON TIMOTHY F; NG SZE-SZE 权利人:JAMISON TIMOTHY F; NG SZE-SZE; MASSACHUSETTS INST TECHNOLOGY 摘要:The present invention relates to new compositions and reactions to produce allylic alcohols or precursors of allylic alcohols (e.g., silyl ethers of allylic alcohols). Methods of the invention may comprise combining an alkene and an aldehyde in the presence of a transition metal catalyst (e.g., a nickel catalyst) to form an allylic alcohol or precursor of an allylic alcohol. Reaction products of the present invention may be valuable as intermediates and/or products in pharmaceutical and polymer research. Also, methods of the invention may be useful as fragment coupling reactions in complex molecule synthesis. Moreover, methods of the invention may include the use of reagents which, under reaction conditions known in the art, may have been unreactive, i.e., may not have been able to form the reaction product. The reagents used in the present invention may be relatively lower in cost than in other methods. Also, methods of the invention may reduce the number of synthetic and purification steps required to produce the reaction products, as well as reducing time, cost, and waste production.
专利号:US-8178559-B2 优先权日:2004-12-30 标 题:Organic compounds 发明人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI 权利人:BREITENSTEIN WERNER; EHARA TAKERU; EHRHARDT CLAUS; GROSCHE PHILIPP; HITOMI YUKO; IWAKI YUKI; KANAZAWA TAKANORI; KONISHI KAZUHIDE; MAIBAUM JUERGEN KLAUS; MASUYA KEIICHI; IWASAKI ATSUKO; OSTERMANN NILS; SUZUKI MASAKI; TOYAO ATSUSHI; YOKOKAWA FUMIAKI; NOVARTIS AG 摘要:3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.
专利号:US-7807709-B2 优先权日:2005-03-23 标题 :Organic compounds 发明人:EHRHARDT CLAUS; IRIE OSAMU; LORTHIOIS EDWIGE LILIANE; MAIBAUM JUERGEN KLAUS; OSTERMANN NILS; SELLNER HOLGER 权利人:NOVARTIS AG 摘要:The invention relates to the use of (3,4-di-, 3,3,4-tri, 3,4,4-tri- or 3,3,4,4-tetra-)substituted pyrrolidine compounds for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; compounds that are part of a subclass of these substituted pyrrolidine compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; new compounds that are part of a subclass of these substituted pyrrolidine compounds; pharmaceutical formulations comprising said substituted pyrrolidine compounds, and/or a method of treatment comprising administering said substituted pyrrolidine compounds, a method for the manufacture especially of said new substituted pyrrolidine compounds, as well as novel intermediates, starting materials and/or partial steps for their synthesis.
专利号:US-9133224-B2 优先权日:2010-11-29 标 题:Macrocyclic kinase inhibitors 发明人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W 权利人:CREW ANDREW P; DONG HANQING; FERRARO CATERINA; SHERMAN DAN; SIU KAM W; OSI PHARMACEUTICALS LLC 摘要:Compounds of Formula (I): wherein variables are defined herein, and pharmaceutically acceptable salts, synthesis, intermediates, formulations, and methods of disease treatment therewith, including cancers for which FAK inhibition is beneficial.
专利号:US-7825149-B2 优先权日:2006-01-19 标 题 :Substituted imidazoles 发明人:CHUBB NATHAN ANTHONY LOGAN; COX MARK ROGER; DAUVERGNE JEROME SEBASTIEN; EWIN RICHARD ANDREW; LAURET CHRISTELLE 权利人:PFIZER LTD 摘要:This invention relates to a range of alpha substituted 2-benzyl substituted imidazole compounds and pharmaceutically acceptable salts and solvates thereof, to compositions comprising such compounds, processes for their synthesis and their use as parasiticides.
专利号:CN-110498915-B 优先权日:2019-07-16 标 题:A simple and controllable synthesis method of α-carboxy-ω-hydroxy polyether
[参考文献]: Alexandra Rotinov, Et Al. Joint Experimental And Theoretical Studies Of The Mechanism For The Gas Phase Elimination Kinetics Of Methyl 2,2-Dimethyl-3-Hydroxypropionate. J Phys Chem A. 2009 Apr 16;113(15):3491-7.
合成参考文献
参考文献:10.1007/s00792-018-1004-0 摘要:Yoneda K, Sakuraba H, Araki T, Ohshima T. Crystal structure of the NADP+ and tartrate-bound complex of L-serine 3-dehydrogenase from the hyperthermophilic archaeon Pyrobaculum calidifontis. Extremophiles. 2018 May;22(3):395–405. doi: 10.1007/s00792-018-1004-0. 参考文献:10.1016/j.jsbmb.2004.03.053 摘要:Fujishima T, Kittaka A, Kurihara M, Saito N, Honzawa S, Kishimoto S, Sugiura T, Waku K, Takayama H. 2,2-Functionalized analogues of 1α,25-dihydroxyvitamin D3, the potent inducers of cell differentiation. The Journal of Steroid Biochemistry and Molecular Biology. 2004 May;89-90():89–92. doi: 10.1016/j.jsbmb.2004.03.053.