2-溴-3-羟基-4-甲氧基苯甲醛置于palladium Diacetate,三苯基膦 Potassium Carbonate,异丙醇体系中,化学反应 14.0H,以82%的收率获得产物异香兰素 参考文献:A Practical Palladium Catalyzed Dehalogenation Of Aryl Halides And α-Haloketones 标题:A Practical Palladium Catalyzed Dehalogenation Of Aryl Halides And α-Haloketones 摘要:A Practical And High-Yielding Protocol For The Dehalogenation Of Aromatic Halides Is Presented. In The Presence Of Palladium Acetate,Triphenylphosphine,And Potassium Carbonate,A Number Of Highly Functionalized Aromatic Halides As Well As Alpha-Haloketones Were Dehalogenated With Alcohols As Hydrogen Donors. (C) 2007 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Tet.2007.03.061
专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
专利号:US-6399776-B2 优先权日:1994-08-05 标题:Processes and intermediates in the synthesis of 5-(3-exo-bicyclo[2.2.1]hept-2-yloxy-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidine-2(1H)-one 发明人:LACOUR THOMAS G; MURTIASHAW III CHARLES WILLIAM 权利人:PFIZER 摘要:This invention relates to novel processes for preparing the pharmaceutically active compound 5-(3-[(2S)-exo-bicyclo[2.2.1]hept-2-yloxy]-4-methoxyphenyl)-3,4,5,6-tetrahydropyrimidin-2(1H)-one and its corresponding 2R enantiomer and for preparing certain intermediates used in the synthesis of these compounds. It also relates to novel intermediates used in the synthesis of such pharmaceutically active compounds and to other novel compounds that are related to such intermediates.
专利号:US-10266565-B2 优先权日:2011-04-12 标 题 :Peptide mimetic ligands of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG-EUN 权利人:BURKE JR TERRENCE R; LIU FA; LEE KYUNG S; PARK JUNG EUN; THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:Novel compounds are provided that bind to polo-like kinases through the polo-box domain. In certain embodiments, the novel compounds are PEGylated peptides. The PEGylated peptides in accordance with the invention demonstrate high PBD-binding affinity. In certain embodiments, the PEGylated peptides have also achieved activities in whole cell systems. The invention also provides compounds that bind polo-like kinases through the polo-box domain and possess reduced anionic charge. Further provided are methods of design and/or synthesis of the PEGylated peptides and methods of use thereof. The invention provides methods of use of the compounds and methods of synthesis of the compounds.
专利号:US-4514569-A 优先权日:1982-01-28 标 题 :Synthesis of 1-substituted isoquinolines 发明人:HENDRICKSON JAMES B; RODRIGUEZ CESAR 权利人:HENDRICKSON JAMES B; RODRIGUEZ CESAR 摘要:A method for the synthesis of particular isoquinoline compounds which are useful intermediates in the preparation of members of the family of opium alkaloids, such as morphine and codeine. Steps in the process include the acylation of the isoquinoline nitrogen; reaction of the acylated isoquinoline with a phosphorous compound; and condensation with a benzaldehyde derivative to yield a 1-benzyl isoquinoline.
专利号:US-8450365-B2 优先权日:2009-05-12 标 题 :Efficient synthesis of galanthamine 发明人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ 权利人:MAGNUS PHILIP D; FAUBER BEN; SANE NEERAJ; UNIV TEXAS 摘要:The present invention relates to methods for the synthesis of galanthamine, morphine, intermediates, salts and derivatives thereof. In preferred embodiments, the invention relates to methods for improving the efficiency and overall yield of said morphine, morphine related derivatives and intermediates thereof. In further embodiments, the invention relates to methods for improving the efficiency and overall yield of galanthamine and intermediates thereof.
专利号:US-7105695-B2 优先权日:2001-12-21 标题 :Synthesis of combretastatin A-2 prodrugs 发明人:PETTIT GEORGE R; MOSER BRYAN R 权利人:UNIV ARIZONA STATE 摘要:The original synthesis of combretastatin A-2 (1a) was modified to provide an efficient scale-up procedure for obtaining this antineoplastic stilbene. Subsequent conversion to a useful prodrug was accomplished by phosphorylation employing in situ formation of dibenzylchlorophosphite followed by cleavage of the benzyl ester protective groups with bromotrimethylsilane to afford phosphoric acid intermediate 11. The latter was immediately treated with sodium methoxide to complete a practical route to the disodium phosphate prodrug (2a). The phosphoric acid precursor (11) of phosphate 2a was employed in a parallel series of reactions to produce a selection of metal and ammonium cation prodrug candidates. Each of the phosphate salts (2a–q) was evaluated with respect to relative solubility behavior, cancer cell growth inhibition, and antimicrobial activity.
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合成参考文献
参考文献:10.1007/s10895-011-0919-y 摘要:Shanker N, Dilek O, Mukherjee K, McGee DW, Bane SL. Aurones: Small Molecule Visible Range Fluorescent Probes Suitable for Biomacromolecules. Journal of Fluorescence. 2011 Jul 12;21(6):2173. doi: 10.1007/s10895-011-0919-y. 参考文献:10.1107/s1600536811016618 摘要:Duan ZY, Ma GL, Yang LP. 4-Meth-oxy-3-(4-nitro-benz-yloxy)benzaldehyde. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1377.