苄氧基三甲基硅烷置于palladium-Platinum,氢气,苯胺体系中,用 N,N-二甲基乙酰胺 用作溶剂,化学反应 2.0H,以97%的收率获得三甲基硅醇 参考文献:Silanol Compound,Composition,And Method For Producing Silanol Compound 标题:Silanol Compound,Composition,And Method For Producing Silanol Compound 摘要:本发明的目的是提供可用作硅氧烷化合物等原料的硅醇化合物,以及硅醇化合物的组合物,并提供一种能够以优异产率生产硅醇化合物的生产方法.通过设计在无水条件下生产硅醇化合物,使用具有抑制硅醇化合物缩合作用的溶剂生产硅醇化合物,并执行其他类似过程,可以制备包含按照(A)至(C)式表示的硅醇化合物质量百分含量为5%至100%的组合物.由于硅醇化合物可以稳定存在于所得组合物中,因此该组合物可用作硅氧烷化合物等的原料.
专利信息
专利号:US-5442065-A 优先权日:1993-09-09 标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A 权利人:UNIV TEXAS 摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
专利号:US-6815214-B2 优先权日:2000-12-29 标 题 :Pharmaceutical uses and synthesis of diketopiperazines 发明人:BOYCE JIM P; HOWBERT J JEFFRY; TABONE JOHN C 权利人:CELLTECH R & D INC 摘要:The synthesis of novel diketopiperazines, their use in inhibiting cellular events such as those involving NFK-α, NFK-β and in the treatment of inflammation events, a combinatorial library of diverse diketopiperazines and process for their synthesis as a library and as individual compounds. In particular novel diketopiperazines are disclosed including their synthesis and use in cellular events such as activation of the transcription factor, nuclear factor, TNF-α, TNF-β and also apoptosis.
专利号:US-2017327504-A1 优先权日:2014-10-30 标 题:Synthesis of Substituted 1H-Pyrazolo[3,4-D]Pyrimidines 发明人:ROSE CHRISTOPHER; SILBERGER HERBERT; SCHREINER ERWIN; FELZMANN WOLFGANG; MARAS NENAD 权利人:SANDOZ AG 摘要:The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H-pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one(ibrutinib) and its synthesis intermediates.
专利号:US-6271379-B1 优先权日:2000-03-08 标题:Intermediates useful for the synthesis of huperzine A 发明人:TUECKMANTEL WERNER; KOZIKOWSKI ALAN P 权利人:UNIV GEORGETOWN 摘要:Intermediates useful for the synthesis of huperzine A represented by the structures below, n and methods for their synthesis, wherein: n R 1 is lower alkyl, benzyl, or substituted benzyl; n X is a suitable leaving group; n Y is an electron withdrawing group that can subsequently be converted into an amino group; n one broken line is present as a carbon—carbon bond and the other broken line is absent, where the broken line forms an unconjugated carbon—carbon double bond, which double bond may be endocyclic whereby n is 3 or the double bond may be exocyclic whereby n is 2.
专利号:US-6844461-B2 优先权日:2001-07-30 标 题:Synthesis of A-ring synthon of 19-NOR-1α,25-dihydroxyvitamin D3 from (D)-glucose 发明人:DELUCA HECTOR F; SHIMIZU MASATO; YAMADA SACHIKO 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides a method for the synthesis of an A-ring synthon phosphine oxide used in the preparation of 19-nor vitamin D compounds, and to novel synthetic intermediates formed during the synthesis. The new method prepares the phosphine oxide from (D)-glucose.
专利号:US-10730904-B2 优先权日:2012-11-14 标 题:Method for liquid-phase synthesis of nucleic acid 发明人:NONOGAWA MITSURU; NAGATA TOSHIAKI; SAITO HIDEKI; YASUMA TSUNEO 权利人:TAKEDA PHARMACEUTICALS CO 摘要:In this method, an oligonucleotide represented by formula (II) [wherein Y 1 , Q, Base, r and r′ are each as defined in claim 1 ] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 and n are each as defined in claim 1 ]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
摘要:Hardman-Baldwin, A. M.; Mattson, A. E., Science of Synthesis Knowledge Updates, (2017) 1, 214. 摘要:Mutoh, Y., Science of Synthesis Knowledge Updates, (2018) 3, 397. 摘要:Chemler, S. R.; Wdowik, T., Science of Synthesis: Catalytic Oxidation in Organic Synthesis, (2017) 1, 362. 参考文献:10.1007/s11745-001-0775-8 摘要:Lyons MA, Brown AJ. Metabolism of an oxysterol, 7-ketocholesterol, by sterol 27-hydroxylase in HepG2 cells. Lipids. 2001 Jul;36(7):701–11. doi: 10.1007/s11745-001-0775-8. 参考文献:10.1107/s1600536810035518 摘要:Grubba R, Baranowska K, Pikies J. catena-Poly[[(tetrahydrofuran-κO)lithium(I)]-bis(μ-trimethylsilanolato-κ2O:O)-gallium(III)-bis(μ-trimethylsilanolato-κ2O:O)-[(tetrahydrofuran-κO)lithium(I)]-μ-bromido]. Acta Crystallogr E Struct Rep Online. 2010 Sep 11;66(10):m1242. doi: 10.1107/s1600536810035518.