合成目标产物 4-Methylanisole 主要起始原料 P-Cresol And Dimethyl Carbonate
(文献来源)合成步骤主要原料 P-Cresol 和 Dimethyl Carbonate
4-甲氧基氯苄置于四(三苯基膦)钯 Diethylzinc体系中,用 正己烷,N,N-二甲基甲酰胺 用作溶剂,化学反应 1.0H,以95%的收率获得对甲苯甲醚 参考文献:Reduction Of Benzylic Halides With Diethylzinc Using Tetrakis(Triphenylphosphine)Palladium As Catalyst 标题:Reduction Of Benzylic Halides With Diethylzinc Using Tetrakis(Triphenylphosphine)Palladium As Catalyst 摘要: Doi:10.1021/jo00076A066
专利信息
专利号:US-9446995-B2 优先权日:2012-05-21 标 题:Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN-SOON; ILLINOIS INST OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
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-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-2022395800-A1 优先权日:2019-11-04 标题:Device for automated synthesis of oligo- and polysaccharides 发明人:SEEBERGER PETER H; DANGLAD FLORES JOSE; LE MAI HOANG KIM; PARDO VARGAS ALONSO; SLETTEN ERIC; SALWICZEK MARIO 权利人:MAX PLANCK GESELLSCHAT ZU RFERDERUNG DER WSS E V; GlycoUniverse GmbH & Co KG&A 摘要:The present invention generally relates to automated synthesis technology, and more particularly, to a device and method for automated synthesis of oligo- and polysaccharides on a solid support. In particular the present invention relates to a device for automated synthesis of oligo- and polysaccharides on a solid support comprising a reaction vessel, a reagent storing component, a reagent delivery system, a cooling device for cooling reaction vessel, and a pre-cooling device for pre-cooling the reagents to be supplied.
专利号:US-7183417-B2 优先权日:2004-04-09 标题:Simple stereocontrolled synthesis of salinosporamide A 发明人:COREY ELIAS J 权利人:HARVARD COLLEGE 摘要:A simple and effective stereocontrolled synthesis of salinosporamide A(1) n nhas been developed which follows the pathway outlined in the FIGURE. The process, the first total synthesis of salinosporamide A, is capable of providing the compound in substantial quantities for further biological studies. In addition to the method of Scheme I, the present invention also includes several novel synthetic intermediate compounds, several intermediate steps of the preferred synthetic process; and the uses of these compounds in the preparation of synthetic derivatives of the compound Salinosporamide A. Salinosporamide A is of special interest as a synthetic target because of its protein in vitro cytotoxic activity against many tumor cell lines (IC 50 values of 10 nM or less).
[参考文献]: Esther F A Brandon, Et Al. Implementation Of Toxicokinetics In Toxicity Studies--Toxicokinetics Of 4-Methylanisole And Its Metabolites In Juvenile And Adult Rats. Regul Toxicol Pharmacol. 2015 Oct;73(1):55-64. [参考文献]: Alessandro Scarso, Et Al. Individual Solvent/solute Interactions Through Social Isomerism. J Am Chem Soc. 2003 Nov 19;125(46):13981-3. [参考文献]: B Brunsborg, Et Al. Four-Week Toxicity Study Of 4-Methoxytoluene In Rats. Toxicol Lett. 1994 Sep;73(3):209-12. [参考文献]: Elisa C M Tonk, Et Al. Developmental Immunotoxicity Testing Of 4-Methyl Anisole. Regul Toxicol Pharmacol. 2015 Jul;72(2):379-85. [参考文献]: H Sakurai, Et Al. Occurrence Of Aromatic Methyl Migration (Nih-Shift) During Oxidation Of P-Methylanisole By Hemin-Thiolester Complex As A Cytochrome P-450 Model. Biochem Biophys Res Commun. 1982 Oct 29;108(4):1649-54.
合成参考文献
参考文献:10.1107/s1600536811012165 摘要:Alen J, Dobrzańska L, Van Meervelt L, De Borggraeve WM. 2-(4-Meth-oxy-benz-yl)-4,6-diphenyl-2,5-diaza-bicyclo-[2.2.2]oct-5-en-3-one. Acta Crystallogr Sect E Struct Rep Online. 2011 May 01;67(Pt 5):o1070–1.