专利号:US-7160517-B2 优先权日:2000-08-18 标题 :Apparatus and methods for the automated synthesis of oligosaccharides 发明人:SEEBERGER PETER H; PLANTE OBADIAH J 权利人:MASSACHUSETTS INST OF TECHNOLG 摘要:One aspect of the present invention relates to an apparatus for the efficient synthesis of oligosaccharides on a solid support, e.g., formed by subunit addition to terminal subunits immobilized on solid-phase particles. In certain embodiments, the apparatus of the present invention is used in combinatorial methods, e.g., as described herein, of synthesizing oligosaccharides.
专利号:US-8822702-B2 优先权日:2002-12-20 标 题 :Synthesis of amines and intermediates for the synthesis thereof 发明人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL 权利人:BERENS ULRICH; DOSENBACH OLIVER; SPRENGER DANIEL; BASF SE 摘要:The invention relates in a first embodiment to a method for the manufacture of esters of the formula I, n nor especially of amides of the formula II,n n nwherein the symbols have the meanings given in the specification, as well as other intermediates and compounds useful in the synthesis of tryptamines and other substances mentioned in the title. The synthesis methods and intermediates are useful in the synthesis of pharmaceuticals.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-7230101-B1 优先权日:2002-08-28 标 题:Synthesis of methotrexate-containing heterodimeric molecules 发明人:MURTHI KRISHNA K; SMITH CHASE C 权利人:GPC BIOTECH INC 摘要:The present invention relates to novel compositions of methotrexate-containing heterodimeric probe molecules, also known as chemical inducers of dimerization (CID), useful in three-hybrid assays. The invention further relates to synthesis of said compositions and their intermediates. Another aspect of the invention is a method for using the heterodimeric probe molecules described herein in drug screens to identify potential protein targets to a given ligand, optimize protein-ligand interactions, or identify potential ligands for a given protein target. In certain embodiments, the invention contemplates the synthesis of the following methotrexate-containing heterodimeric probe:
专利号:US-6770436-B1 优先权日:1996-11-14 标题:Chemical amplification for the synthesis of patterned arrays 发明人:BEECHER JODY E; GOLDBERG MARTIN J; MCGALL GLENN H 权利人:AFFYMETRIX INC 摘要:Radiation-activated catalysts (RACs), autocatalytic reactions, and protective groups are employed to achieve a highly sensitive, high resolution, radiation directed combinatorial synthesis of pattern arrays of diverse polymers. When irradiated, RACs produce catalysts that can react with enhancers, such as those involved in autocatalytic reactions. The autocatalytic reactions produce at least one product that removes protecting groups from synthesis intermediates. This invention has a wide variety of applications and is particularly useful for the solid phase combinatorial synthesis of polymers.
专利号:US-8569560-B2 优先权日:2006-10-13 标题 :Synthesis of terminal alkenes from internal alkenes via olefin metathesis 发明人:SCHRODI YANN; PEDERSON RICHARD L; KAIDO HIROKI; TUPY MICHAEL J 权利人:ELEVANCE RENEWABLE SCIENCES 摘要:This disclosure relates generally to olefin metathesis, and more particularly relates to the synthesis of terminal alkenes from internal alkenes using a cross-metathesis reaction catalyzed by an olefin metathesis catalyst. According to one aspect, for example, a method is provided for synthesizing a terminal olefin, the method comprising contacting, in the presence of a ruthenium alkylidene metathesis catalyst, an olefinic substrate comprised of at least one internal olefin with a cross metathesis partner comprised of an alpha olefinic reactant, under reaction conditions effective to allow cross-metathesis to occur, wherein the reaction conditions include a reaction temperature of at least 35° C. The methods, compositions, reactions and reaction systems herein disclosed have utility in the fields of catalysis, organic synthesis, and industrial chemistry.
1: Zhang JX, Guo JM, Zhang TT, Lin HJ, Qi NS, Li ZG, Zhou JC, Zhang ZZ. Antiproliferative Phenothiazine Hybrids as Novel Apoptosis Inducers against MCF-7 Breast Cancer. Molecules. 2018 May 28;23(6). pii: E1288. doi: 10.3390/molecules23061288. doi: 10.1016/j.ijbiomac.2018.03.074. Epub 2018 Mar 16. doi: 10.1691/ph.2018.7806. doi: 10.3389/fnmol.2017.00447. eCollection 2017. 7: Zhang J, Ming C, Zhang W, Okechukwu PN, Morak-Młodawska B, Pluta K, Jeleń M, Akim AM, Ang KP, Ooi KK. 10H-3,6-Diazaphenothiazine induces G(2)/M phase cell cycle arrest and caspase-dependent apoptosis and inhibits cell invasion of A2780 ovarian carcinoma cells through the regulation of NF-κB and (BIRC6-XIAP) complexes. Drug Des Devel Ther. 2017 Oct 24;11:3045-3063. doi: 10.2147/DDDT.S144415. eCollection 2017. 8: Varga B, Csonka Á, Csonka A, Molnár J, Amaral L, Spengler G. Possible Biological and Clinical Applications of Phenothiazines. Anticancer Res. 2017 Nov;37(11):5983-5993. Review. doi: 10.1007/s00044-017-1944-4. Epub 2017 Jun 15.
合成参考文献
参考文献:10.2116/analsci.27.727 摘要:Li Y, Yang W, Fan M, Liu A. A Sensitive Label-free Amperometric CEA Immunosensor Based on Graphene-Nafion Nanocomposite Film as an Enhanced Sensing Platform. Analytical Sciences. 2011 Jul 10;27(7):727–31. doi: 10.2116/analsci.27.727. 摘要:Takács D, Cerca P, Martins A, Riedl Z, Hajós G, Molnár J, Viveiros M, Couto I, Amaral L. Evaluation of forty new phenothiazine derivatives for activity against intrinsic efflux pump systems of reference Escherichia coli, Salmonella Enteritidis, Enterococcus faecalis and Staphylococcus aureus strains. In Vivo. 2011 Sep;25(5):719–24. 参考文献:10.1016/j.jpba.2005.10.035 摘要:Wójciak-Kosior M, Skalska A, Matysik A. Determination of phenothiazine derivatives by high performance thin-layer chromatography combined with densitometry. Journal of Pharmaceutical and Biomedical Analysis. 2006 Apr;41(1):286–9. doi: 10.1016/j.jpba.2005.10.035. 参考文献:10.1038/cddis.2011.62 摘要:Zong D, Hååg P, Yakymovych I, Lewensohn R, Viktorsson K. Chemosensitization by phenothiazines in human lung cancer cells: impaired resolution of γH2AX and increased oxidative stress elicit apoptosis associated with lysosomal expansion and intense vacuolation. Cell Death & Disease. 2011 Jul 21;2(7):e181. doi: 10.1038/cddis.2011.62. 参考文献:10.1371/journal.pone.0021966 摘要:Wu J, Song R, Song W, Li Y, Zhang Q, Chen Y, Fu Y, Fang W, Wang J, Zhong Z, Ling H, Zhang L, Zhang F. Chlorpromazine Protects Against Apoptosis Induced by Exogenous Stimuli in the Developing Rat Brain. PLoS ONE. 2011 Jul 14;6(7):e21966. doi: 10.1371/journal.pone.0021966.