CAS: 900515-16-4; (Z)-5-((5-(4-Fluoro-2-Hydroxyphenyl)Furan-2-yl)Methylene)Thiazolidine-2,4-Dione

上下游产品

5-(4-fluoro-2-hydroxyphenyl)furan-2-carbaldehyde thiazoline-2,4-dione 2-Benzyloxy-1-bromo-4-fluoro-benzene 5-(2-benzyloxy-4-fluorophenyl)furan-2-carbaldehyde

2-溴-5-氟苯酚置于四(三苯基膦)钯,Potassium Carbonate,溶剂黄146,β-丙氨酸体系中,用 乙醇,甲苯 作为反应溶剂,化学反应 13.0H,反应生成 5-[[5-(4-氟-2-羟基苯基)-2-呋喃基]亚甲基]-2,4-噻唑烷二酮
参考文献:Furan-2-Ylmethylene Thiazolidinediones As Novel,Potent,And Selective Inhibitors Of Phosphoinositide 3-Kinase γ
标题:Furan-2-Ylmethylene Thiazolidinediones As Novel,Potent,And Selective Inhibitors Of Phosphoinositide 3-Kinase γ
摘要:Class I Phosphoinositide 3-Kinases (Pi3Ks),In Particular Pi3K Gamma,Have Become Attractive Drug Targets For Inflammatory And Autoimmune Diseases. Here,We Disclose A Novel Series Of Furan-2-Ylmethylene Thiazolidinediones As Selective,Atp-Competitive Pi3K Gamma Inhibitors. Structure-Based Design And X-Ray Crystallography Of Complexes Formed By Inhibitors Bound To Pi3K Gamma Identified Key Pharmacophore Features For Potency And Selectivity. An Acidic Nh Group On The Thiazolidinedione Moiety And A Hydroxy Group On The Furan-2-Yl-Phenyl Part Of The Molecule Play Crucial Roles In Binding To Pi3K And Contribute To Class Ib Pi3K Selectivity. Compound 26 (As-252424),A Potent And Selective Small-Molecule Pi3K Gamma Inhibitor Emerging From These Efforts,Was Further Profiled In Three Different Cellular Pi3K Assays And Shown To Be Selective For Class Ib Pi3K-Mediated Cellular Effects. Oral Administration Of 26 In A Mouse Model Of Acute Peritonitis Led To A Significant Reduction Of Leukocyte Recruitment.
DOI:10.1021/jm0601598

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

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-2023192682-A1
优先权日:2019-11-14
标题:Improved synthesis of kras g12c inhibitor compound

专利号:US-2023192681-A1
优先权日:2019-11-14
标 题 :Improved synthesis of kras g12c inhibitor compound

专利号:WO-2020102730-A1
优先权日:2018-11-16
标 题:Improved synthesis of key intermediate of kras g12c inhibitor compound