合成目标产物 Methyl Thioglycolate 主要起始原料 Methanol And Thioglycolic Acid
(文献来源)合成步骤主要原料 Methanol 和 Thioglycolic Acid
二甲基2,2'-二硫烷二基二乙酸酯置于magnesium体系中,用 甲醇 用作溶剂,化学反应 2.0H,以85%的收率获得巯基乙酸甲酯 参考文献:Reduction Of Symmetric Disulfides To Thiols Using Mg In Methanol∗ 标题:Reduction Of Symmetric Disulfides To Thiols Using Mg In Methanol∗ 摘要:An Efficient Reduction Of Disulfides To Thiols Using Mg In Methanol Described. Doi:10.1080/00397919708006063
专利号:US-11220513-B2 优先权日:2015-04-30 标题:Chromium-mediated coupling and application to the synthesis of halichondrins 发明人:KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO 权利人:HARVARD COLLEGE 摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
专利号:US-6096898-A 优先权日:1999-10-22 标 题:One pot synthesis of 1,2,4-triazoles 发明人:PODHOREZ DAVID E; HULL JR JOHN W; BRADY CHRISTINE H 权利人:DOW AGROSCIENCES LLC 摘要:One pot synthesis of 1,2,4-triazoles uses thioimidate intermediate and 1,2-dichloroethane solvent.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-8471010-B2 优先权日:2008-05-13 标题:Synthesis of dihydrothieno[3,2-d]pyrimidine diols 发明人:FRUTOS ROGELIO P; TAMPONE THOMAS G; MULDER JASON ALAN; KRISHNAMURTHY DHILEEPKUMAR; SENANAYAKE CHRIS H 权利人:FRUTOS ROGELIO P; TAMPONE THOMAS G; MULDER JASON ALAN; KRISHNAMURTHY DHILEEPKUMAR; SENANAYAKE CHRIS H; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to an improved process for the preparation of dihydrothieno[3,2-d]pyrimidine diols, and similar pyrimidine diols, that is efficient, high-yielding, and does not require expensive and potentially unstable intermediates. The diols are used as intermediates in the synthesis of pyrimidine compounds which inhibit PDE4, and are thus useful in the treatment of respiratory or gastrointestinal diseases and complaints, peripheral or central nervous system diseases and disorders, inflammatory conditions, and cancers.
专利号:US-11524957-B2 优先权日:2018-04-02 标 题 :Process for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one 发明人:ZHU LEI; BAILEY JOHN DANIEL; DURAK LANDON; WAETZIG JOSHUA DAVID; MIZUNO MASAHIRO; MAEDA KAZUHIRO; YASUMA TSUNEO; YAMAGUCHI HIROSHI; FUKUOKA KOICHIRO; AKIYAMA KAZUYUKI 权利人:TAKEDA PHARMACEUTICALS CO 摘要:The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.
专利号:US-5693848-A 优先权日:1994-10-21 标题:α, ω-polymethacrylate dicarboxylic acids, their synthesis and use as dicarboxylic acid components for the synthesis or modification of polyesters, polyurethanes or polyepoxides 发明人:ESSELBORN EBERHARD; FOCK JUERGEN 权利人:GOLDSCHMIDT AG TH 摘要:alpha , omega -polymethacrylate dicarboxylic acids of the general formula wherein R1is an optionally halogenated alkyl group with 1 to 22 carbon atoms, wherein the R1 group can assume different meanings in the polymer molecule, R2 is the group of a known chain transfer agent, which has a terminal -COOH croup and a has a value not less than 4. The invention furthermore relates to the synthesis of these compounds and their use as sole or partial components for the synthesis or modification of polyepoxides, polyesters, polyamides, alkyd resins or polyurethanes.
参考标题:Catalyst-Controlled Regiodivergent Synthesis Of 1- And 3-Thiosugars With High Stereoselectivity And Chemoselectivity 作者:Yuexin Liu,Yang Jiao,Huajun Luo,Nianyu Huang,Mengnan Lai,Kun Zou,Hui Yao |发布日期:2021.5.7 摘要:An Effective Regiodivergent Synthesis Toward 1- And 3-Thiosugars Was Achieved Through Palladium And Cobalt Catalysis, Respectively. β-1-Thiosugars Were Obtained From 3,4-O-Carbonate-Glycals And Various Thiols Catalyzed By Pd2(Dba)3 In Good Yields With Exclusive Stereoselectivity And Chemoselectivity, While Only (3S)-3-Thiosugars Were Generated Via Co(Bf4)2. Experiments And Dft Calculations Supported
合成参考文献
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 68. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 293. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 304. 摘要:von Angerer, S., Science of Synthesis Knowledge Updates, (2011) 1, 403. 摘要:Landelle, G.; Paquin, J.-F., Science of Synthesis Knowledge Updates, (2010) 4, 278.