CAS: 871700-17-3; N-(3-(3-Cyclopropyl-5-((2-Fluoro-4-Iodophenyl)Amino)-6,8-Dimethyl-2,4,7-Trioxo-3,4,6,7-Tetrahydropyrido[4,3-D]Pyrimidin-1(2H)-yl)Phenyl)Acetamide

上下游产品

N-{3-[3-cyclopropyl-1-(2-fluoro-4-iodophenyl)-6,8-dimethyl-2,4,7-trioxo-1,2,3,4,7,8-hexahydropyrido[2,3-d]pyrimidin-5-ylamino]phenyl}acetamide N-(2-fluoro-4-iodophenyl)-N'-methylurea 2-fluoro-4-iodo-N-((methylimino)methylene)aniline ethyl 2-(2-fluoro-4-iodophenylamino)-4-hydroxy-1,5-dimethyl-6-oxo-1,6-dihydropyridine-3-carboxylate

1-(2-Fluoro-4-Iodophenyl)-3-Methylurea置于吡啶,Sodium Dithionite,四溴化碳,Sodium Ethanolate,乙酸酐,三乙胺,三苯基膦体系中,用 四氢呋喃,二氯甲烷,氯仿,水,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 33.0H,反应生成 曲美替尼
参考文献:一种合成曲美替尼的方法
标题:一种合成曲美替尼的方法
摘要:本发明公开了一种曲美替尼的合成方法,采用n‑(2‑氟‑4‑碘苯基)‑n'‑甲基脲脱水成碳二亚胺后,与2‑甲基‑3‑氧代‑戊二酸二乙酯进行环合反应得2‑(2‑氟‑4‑碘苯基氨基)‑4‑羟基‑1,5‑二甲基‑6‑氧代‑1,6‑二氢吡啶‑3‑羧酸乙酯;然后与n‑(3‑硝基苯基)‑n'‑环丙基脲进行环合得3‑环丙基‑5‑(2‑氟‑4‑碘苯基氨基)‑6,8‑甲基‑1‑(3‑硝基苯基)吡啶并[4,3‑d]嘧啶‑2,4,7(1H,3H,6H)‑三酮;最后先还原硝基,再进行乙酰化即得曲美替尼.本发明通过逆合成分析,提出了一种曲美替尼的合成新路线,可以大大缩短工艺流程,且制备过程中未使用昂贵试剂,具有操作简便,成本较低的优势,为曲美替尼的制备提供了参考.

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-2022233673-A1
优先权日:2019-06-04
标 题:METHODS OF PRODUCING SHIGA TOXIN B-SUBUNIT (STxB) MONOMERS AND OLIGOMERS, AND USES THEREOF
发明人：BILLET ANNE; SCHMIDT FRÉDÉRIC; JOHANNES LUDGER; SERVENT DENIS; MOURIER GILLES; TARTOUR ÉRIC; KAY MICHAEL; FULCHER JAMES M
权利人:INST CURIE; CENTRE NAT RECH SCIENT; INST NAT SANTE RECH MED; COMMISSARIAT A LENERGIE ATOMIQUE ET AUX ENERGIES ALTERNATIVES CEA; APHP ASSIST PUBLIQUE HOPITAUX DE PARIS; UNIV PARIS; UNIV OF UTAH RESEARCH FOUDATION; UNIV UTAH RES FOUND
摘要:A method of producing a monomer of a Shiga toxin B-subunit (STxB) protein or of a variant thereof by peptide chemical synthesis, as well as to a method of producing a pentamer of the STxB protein or of the variant thereof. The methods are particularly advantageous as they overcome major issues typically observed in peptide chemical synthesis, including solubility and purity issues.

专利号:US-2024400519-A1
优先权日:2023-06-01
标 题 :Crystal forms a, b, c, d, e, f and g of selumetinib sulfate and preparation methods thereof
发明人：HSU YAO-LUNG; HSIEH KUANG-CHAN; CHENG HUI-WEN; Yang zong-han
权利人:CHUNGHWA CHEMICAL SYNTHESIS & BIOTECH CO LTD
摘要:The present invention relates to crystal forms of A, B, C, D, E, F and G of selumetinib sulfate and the preparation method thereof. The crystal forms A, B and F of selumetinib sulfate are obtained by adding 6-(4-Bromo-2-chloro-phenylamino)-7-fluoro-3-methyl-3H-benzoimidazole-5-carboxylic acid (2-vinyloxy-ethoxy)-amide (SEL-3) into an organic solvent; further, crystal form A of selumetinib sulfate can be as a raw material to prepare crystal forms C, D and E of selumetinib sulfate, and crystal form C of selumetinib sulfate can be as a raw material to prepare crystal form G of selumetinib sulfate.

专利号:US-11612610-B2
优先权日:2018-12-14
标题:Mito-magnolol compounds and methods of synthesis and use thereof
发明人：KALYANARAMAN BALARAMAN; ZIELONKA JACEK MICHAL; CHENG GANG; HARDY MICAEL JOËL; OUARI OLIVIER
权利人:MEDICAL COLLEGE WISCONSIN INC; AIX MARSEILLE UNIV; MEDICAL COLLEGE OF WISCONSIN INC
摘要:The present invention provides mito-magnolol compounds, pharmaceutical compositions thereof, and methods of using the mito-magnolol compounds in the treatment of cancer, especially anti-cancer therapy or kinase resistant cancers.

专利号:US-2022118094-A1
优先权日:2019-02-21
标题:Synthesis of biomimetic cell wall structure
发明人：WANG YONG; SHI PENG
权利人:PENN STATE RES FOUND
摘要:The present invention relates generally to methods of generating a biomimetic cell wall (BCW) on a target surface, compositions comprising the BCW, and methods of use of the compositions, including biomedical applications of the BCW coated compositions.