CAS: 257933-82-7; (E)-N-(4-((3-Chloro-4-Fluorophenyl)Amino)-3-Cyano-7-Ethoxyquinolin-6-yl)-4-(Dimethylamino)But-2-Enamide

上下游产品

4-brom°Crotonyl chloride dimethyl amine 6-amino-4-(3-chloro-4-fluoro-phenylamino)-7-ethoxy-quinoline-3-carbonitrile (2E)-(N,N-dimethylamino)-2-butenoyl chloride

(E)-2-Cyano-3-(3-Ethoxy-4-Nitro-Phenylamino)-Acrylic Acid Ethyl Ester置于diphenyl Ether-Biphenyl Eutectic,铁粉,氯化铵,N,N-二异丙基乙胺,三氯氧磷体系中,用 四氢呋喃,甲醇,异丙醇 用作溶剂,化学反应 11.25H,反应生成培利替尼
参考文献:Synthesis And Structure−activity Relationships Of 6,7-Disubstituted 4-Anilinoquinoline-3-Carbonitriles. The Design Of An Orally Active,Irreversible Inhibitor Of The Tyrosine Kinase Activity Of The Epidermal Growth Factor Receptor (Egfr) And The Human Epidermal Growth Factor Receptor-2 (Her-2)
标题:Synthesis And Structure−activity Relationships Of 6,7-Disubstituted 4-Anilinoquinoline-3-Carbonitriles. The Design Of An Orally Active,Irreversible Inhibitor Of The Tyrosine Kinase Activity Of The Epidermal Growth Factor Receptor (Egfr) And The Human Epidermal Growth Factor Receptor-2 (Her-2)
摘要:A Series Of Of 6,7-Disubstituted-4-Anilinoquinoline-3-Carbonitrile Derivatives That Function As Irreversible Inhibitors Of Egfr And Her-2 Kinases Have Been Prepared. These Inhibitors Have,At The 6-Position,Butynamide,Crotonamide,And Methacrylamide Michael Acceptors Bearing Water-Solublilizing Substituents. These Compounds Were Prepared By Acylation Of 6-Amino-4-(Arylamino)Quinoline-3-Carbonitriles With Unsaturated Acid Chlorides Or Mixed Anhydrides. We Performed Competitive Reactivity Studies Showing That Attaching A Dialkylamino Group Onto The End Of The Michael Acceptor Results In Compounds With Greater Reactivity Due To Intramolecular Catalysis Of The Michael Addition. This,Along With Improved Water-Solubility Results In Compounds With Enhanced Biological Properties. We Present Molecular Modeling Results Consistent With The Proposed Mechanism Of Inhibition. One Compound,5 (Ekb-569),Which Shows Excellent Oral In Vivo Activity,Was Selected For Further Studies And Is Currently In Phase I Clinical Trials For The Treatment Of Cancer.
Doi:10.1021/jm020241C

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-7126025-B2
优先权日:2003-01-21
标 题 :Synthesis of 4-(amino)-2-butenoyl chlorides and their use in the preparation of 3-cyano quinolines
发明人：CONSIDINE JOHN LEO; DAIGNEAULT SYLVAIN; CHEW WARREN; IERA SILVIO; DUNCAN SCOTT MASON; REN JIANXIN
权利人:WYETH CORP
摘要:This invention provides a compound of Formula (I): n nwhereinn S 1 and S 2 are each independently, hydrogen, alkyl, alkenyl, alkynyl, aralkyl, substituted or unsubstituted aryl, and S 1 and S 2 together with the nitrogen to which they are attached form a nitrogen containing heteroaryl and a pharmaceutically acceptable salt thereof; a method of preparing the compound of Formula (I), and use of the compound of Formula (I) in the preparation of 3-cyano quinolines.

专利号:US-7294740-B2
优先权日:2002-02-05
标 题:Process for the synthesis of N-acyl-2-amino-4-alkoxy-5-nitrobenzoic acids
发明人：DUNCAN SCOTT MASON; OSUMA AUGUSTINE TOBI; DAIGNEAULT SYLVAIN; BERNATCHEZ MICHEL
权利人:WYETH CORP
摘要:The invention claimed herein provides a process to oxidize N-(5-alkoxy-2-methyl-4-nitrophenyl)acetamides to N-acyl-2-amino-4-alkoxy-5-nitrobenzoic acids using potassium permanganate in the presence of magnesium sulfate in aqueous sulfolane or aqueous pyridine.

专利号:US-2025289827-A1
优先权日:2022-12-02
标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof
发明人：YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN
权利人:C4 THERAPEUTICS INC
摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.

专利号:US-2006078560-A1
优先权日:2003-06-23
标 题 :Method of inducing apoptosis and inhibiting cardiolipin synthesis
发明人：JAMIL HARIS; AHMAD MOGHIS U; AHMAD IMRAN
权利人:NEOPHARM INC
摘要:The present invention provides a method for inducing apoptosis within a cell by exposing the cell to an inhibitor of cardiolipin synthesis under conditions sufficient to induce apoptosis within the cell. The method can be used to investigate or treat disorders such as cancer, obesity, and cardiovascular disorders. The invention also provides a pharmaceutical composition including an inhibitor of cardiolipin synthesis and a liposomal carrier.