专利号:US-9765077-B2 优先权日:2015-05-29 标题:Synthesis of duocarmycin analogues 发明人:STEPHENSON MICHAEL J; HOWELL LESLEY A; SEARCEY MARK 权利人:UNIV OF EAST ANGLIA 摘要:A novel Fmoc protected duocarmycin subunit and utilization as a reagent in solid phase protein synthesis methodology. Also provided is a novel method of solid phase peptide synthesis, and in particular a method for the production of novel intermediates and novel monomeric and extended duocarmycin analogues having amino acid substituents.
专利号:US-6310209-B1 优先权日:1997-12-08 标题:Synthesis of CC-1065/duocarmycin analogs 发明人:BOGER DALE L 权利人:SCRIPPS RESEARCH INST 摘要:The present invention relates to a method for the synthesis of the dihydroindole C-ring found in CC-1065/duocarmycin analogs.
专利号:US-7365203-B2 优先权日:2003-09-15 标题:Process for the synthesis of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile 发明人:DAIGNEAULT SYLVAIN; MICHALAK RONALD STANLEY; BERNATCHEZ MICHEL 权利人:WYETH CORP 摘要:The present invention provides a process for the preparation of 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile comprising the steps and products disclosed within this application.
专利号:US-4005067-A 优先权日:1970-10-28 标题 :Process for the synthesis of nitrite ion-containing 1:1 complexes of cobalt and metallizable monoazo or azomethine compounds and such complexes 发明人:DORE JACKY 权利人:SANDOZ LTD 摘要:By metallization of metallizable monoazo or azomethine dyes with cobalt-donating compounds in the presence of a nitrite, especially NaNO 2 , 1:1 cobalt complexes containing a nitrite ion are obtained in a high degree of metallization which can be reacted with metallizable monoazo or azomethine dyes to give very homogeneous 2:1 cobalt complexes in a high degree of purity. This is particularly advantageous when asymmetrical 2:1 cobalt complexes are to be prepared. The process is particularly useful for the preparation of nitrite ion-containing 1:1 complexes of cobalt and a monoazo compound of the formula ##STR1## wherein X is --OH or --NHR, n wherein R is hydrogen or a substituted or unsubstituted alkyl, cycloalkyl, phenyl or naphthyl group, n Ring A is further unsubstituted or further substituted by at least one halo, nitro or optionally substituted alkyl, alkoxy or sulfamoyl substituent, and n The naphthalene ring is further unsubstituted or further substituted by at least one hydroxy, sulfamoyl or acylamino substituent.
专利号:US-2016194279-A1 优先权日:2012-12-09 标 题 :One pot process for the conversion of aroyl chlorides to acyl thioureas 发明人:CHEPURI VENKATA RAMANA; BEERAN SENTHILKUMAR 权利人:COUNCIL SCIENT IND RES 摘要:The present invention disclose an improved one pot process for synthesis of acyl thioureas of formula (I), with yield greater than 80%, from aroyl chlorides of formula (I) wherein, R′ is an aryl or a heteroarylene group substituted with one or more groups selected from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino, carboxyl, ester, halogenated hydrocarbon or an aryl or heteroaryl; R″ and R′″ are selected independently from hydrogen, alkyl, alkylene, alkynyl, alkoxy, alkenyloxy, halo, hydroxyl, nitro, amino or halogenated hydrocarbon.
专利号:US-7550510-B2 优先权日:2001-07-06 标 题 :Solid phase synthesis of arylretinamides 发明人:CURLEY JR ROBERT W; MERSHON SERENA M; BARNETT DEREK W; CLAGETT-DAME MARGARET; CHAPMAN JASON S 权利人:WISCONSIN ALUMNI RES FOUND 摘要:A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.
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