肉桂酸置于5%-Palladium/activated Carbon,氢气,双氧水,Sodium Methylate,乙酸酐,Potassium Hydroxide体系中,用 四氢呋喃,甲醇,水,甲苯 作为反应溶剂,化学反应 47.0H,反应生成 高邻苯二甲酸酐 参考文献:Synthesis And Antitumor Activity Evaluation Of 2-Arylisoquinoline-1,3(2H,4H)-Diones In Vitro And In Vivo 标题:Synthesis And Antitumor Activity Evaluation Of 2-Arylisoquinoline-1,3(2H,4H)-Diones In Vitro And In Vivo 摘要:Six 2-(2-Acylaminobenzothiazol-6-yl)Isoquinoline-1,3(2H,4H)-Diones (1A-1F) And Five 2-Arylisoquinoline-1,3(2H,4H)-Diones (1G-1K) Were Synthesized By Refluxing Homophthalic Anhydrides With 2-Acylaminobenzothiazolyl-6-Amine Or Substituted Aniline In Glacial Acetic Acid. The Cytotoxic Activities Of 1A-1K Were Evaluated Via Mtt Method Against A431,A549,And Pc3. Compound 1B Relatively Displayed A Higher Cytotoxic Activity Than The Others. The Antitumor Effect Of 1B Were Evaluated In Established Nude Mice Panc-1 Xenograft Model. The Results Suggest That Compound 1B Could Potentially Inhibit Tumor Growth. DOI:10.1007/s00044-013-0734-X
专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
专利号:US-2012189547-A1 优先权日:2009-10-08 标 题 :[18f] labelled analogues of flumazenil as in vivo imaging agents 发明人:WOODCRAFT JOHN; JONES CLARE L; GAETA ALESSANDRA; TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER; PLANT STUART 权利人:WOODCRAFT JOHN; JONES CLARE L; GAETA ALESSANDRA; TRIGG WILLIAM JOHN; JONES PAUL ALEXANDER; PLANT STUART 摘要:The present invention provides radiofluorinated compounds useful for in vivo imaging GABA A receptors. Also provided by the present invention is a method of synthesis for the radiofluorinated compounds of the invention, in particular an automated method of synthesis. A further aspect of the invention is a cassette suitable for carrying out the automated method of synthesis of the invention.
专利号:US-6121054-A 优先权日:1997-11-19 标 题 :Method for separation of liquid and solid phases for solid phase organic syntheses 发明人:LEBL MICHAL 权利人:TREGA BIOSCIENCES INC 摘要:A simple, efficient apparatus and method for separation of solid and liquid phases useful in methods of high-throughput combinatorial organic synthesis of large libraries or megaarrays of organic compounds is disclosed. The apparatus and method are useful, whether as part of an automated, robotic or manual system for combinatorial organic synthesis. In a preferred embodiment, an apparatus and method of removal of liquid phase from solid phase compatible with microtiter plate type array(s) of reaction vessels is disclosed.
专利号:US-9969686-B2 优先权日:2014-08-05 标 题 :Synthesis of diindolylmethanes and indolo[3,2-b]carbazoles, compounds formed thereby, and pharmaceutical compositions containing them 发明人:TANG WEIPING; LI XIAOXUN; SHU DONGXU; WINSTON-MCPHERSON GABRIELLE N 权利人:WISCONSIN ALUMNI RES FOUND 摘要:Described is a method to make diindolylmethanes and indolyl/pyrrolylmethanes, The method includes the steps of contacting an ether comprising an arylpropargyl moiety and an amine-protected, substituted or unsubstituted aniline moiety with a substituted or unsubstituted indol or a substituted or unsubstituted pyrrole, in the presence of a metal-containing catalyst, for a time and at a temperature to cause an annulation/arylation cascade reaction that yields a diindolylmethane or a indolyl/pyrrolylmethane. The resulting compounds are effective to modulate activity of arylhydrocarbon receptors, to inhibit activity of PCSK9, and to stimulate secretion of glucagon-like peptide 1 in mammals.
专利号:US-2023357257-A1 优先权日:2020-12-28 标 题 :Novel process for the synthesis of noroxymorphone from morphine 发明人:GORBACHEV DMITRY; LAM HON WAI; SAXENA AAKARSH; SAXENA NAVIN SATYAPAL 权利人:NAVIN SAXENA RESEARCH & TECH PVT LTD 摘要:The present invention relates to a novel, efficient, pot- and atom-economical, and industrially applicable process for converting morphine to noroxymorphone using reagents and solvents of lesser toxicity and lower cost with respect to those used in the prior art.
专利号:US-3708477-A 优先权日:1968-06-27 标 题:Process of total synthesis of cephalosporin derivatives and intermediates 发明人:MARTEL J; HEYMES R 权利人:ROUSSEL UCLAF 摘要:PROCESS FOR THE PREPARATION OF RACEMIC OR OPTICALLYACTIVE CEPHALOSPORINE DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-NH2-2-CEPHEM WHEREIN R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, SUBSTITUTED AKYL, ARYL AND SUBSTITUTED ARYL, WHICH COMPRISES THE STEPS OF REACTING AN AMINO ACID OF THE FORMULA R1-NH-CH2-CH2-COOH WITH BENZYL ALCOHOL, CONDENSING THE BENZYL ESTER THUS OBTAINED WITH AN OXALATE, CONVERTING THE BENZYL ESTER OF 2,3DIOXI-4-CARBOXY-PYRROLIDINE INTO THE CORRESPONDING ACID, SUBJECTING SAID ACID TO AMINOMETHYLATION, THUS YIELDING A COMPOUND OF THE FORMULA 1-R1,3-OH,4-(R'-N(-R'')-CH2-)PYRROL-3-IN-2-ONE CONVERTING SAID COMPOUND INTO THE CORRESPONDING 4-ACYLTHIOMETHYL DERIVATIVE, CONVERTING SAID DERIVATIVE INTO THE CORRESPONDING 4-THIOMETHYL DERIVATIVE, CONDENSING SAID DERIVATIVE WITH AN ENAMINE OF THE FORMULA R-OOC-C(-Y)=CH-NH2 TO OBTAIN A THIAZINE DERIVATIVE OF THE FORMULA 2-(Y-CH(-COO-R)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-D)-1,3-THIAZIN-4-ONE CONVERTING SAID THIAZINE DERIVATIVE INTO A COMPOUND OF THE FORMULA 2-(H2N-CH(-COOH)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-)-1,3-THIAZIN-4-ONE SUBJECTING SAID COMPOUND TO THE ACTION OF A TRITYLATION AGENT, RECOVERING THE THREO ISOMER OF THE TRITYLATED DERIVATIVE, LACTAMIZING SAID THREO ISOMER TO OBTAIN THE Y-LACTAM OF DL-6H,7H-CIS-7-TRITYLAMINO-3-AMINOALKYL-CEPH 3-EME-4-CARBOXYLIC ACID, DETRITYLATING SAID Y-LACTAM AND RECOVERING SAID RACEMIC OF OPTICALLY ACTIVE CEPHALOSPORIN DERIVATIVES. THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF THE CORRESPONDING 7ACYLAMINO DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-(R2-NH-)-2-CEPHEM WHEREIN R1 HAS THE ABOVE DEFINITION AND R2 IS THE ACYL OF AN ORGANIC CARBOXYLIC ACID WHICH COMPOUNDS ARE ALSO PART OF THE INVENTION AND ARE USEFUL AS ANTIBIOTICS.
[参考文献]: Ali A Mohammadi, Et Al. Multicomponent One-Pot Reactions: Synthesis Of Some New 6-Oxopyrano [2,3-C]Isochromenes By Condensation Of Homophthalic Anhydride, Dialkyl Acetylenedicarboxylate, And Isocyanides. Comb Chem High Throughput Screen. 2009 Jun;12(5):536-42.
合成参考文献
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