CAS: 110690-43-2; 6-(Benzoyloxy)-3-Cyanopyridin-2-Yl 3-(3-(Ethoxymethyl)-5-Fluoro-2,6-Dioxo-1,2,3,6-Tetrahydropyrimidine-1-Carbonyl)Benzoate

上下游产品

6-benzoyloxy-3-cyano-2-pyridone 1-ethoxymethyl-5-fluorouracil benzoyl chloride 3-cyano-2,6-dihydroxypyridine

📜1,2-二氢-6-羟基-2-氧代-3-氰基吡啶置于三乙胺体系中,用 氯仿,N,N-二甲基乙酰胺 用作溶剂,化学反应 3.0H,反应生成乙嘧替氟
参考文献:Synthesis Of 5-Fluorouracil Derivatives Containing An Inhibitor Of 5-Fluorouracil Degradation.
标题:Synthesis Of 5-Fluorouracil Derivatives Containing An Inhibitor Of 5-Fluorouracil Degradation.
摘要:研究了 5-氟尿嘧啶(5-Fura)降解抑制剂 2,4-(2)和 2,6-二羟基吡啶(3)的反应活性.2 和 2,4-双(三甲基硅氧基)吡啶分别在 4-Oh 和 2-Oh 位优先与等摩尔量的酸氯发生酰化反应,通过 X 射线晶体图分析确定单苯甲酰化 5-氯-2,4-二羟基吡啶 (2B) 的结构为 4-苯甲酰基氧基-5-氯-2-吡啶酮 (5B).化合物 2 和 3 以及 2 的 N-2-四氢糠基(11),N-烷基(12)和 N-氨基甲酰基(14)衍生物表现出动态的酮烯醇同分异构现象.这些吡啶的酰基衍生物具有易变性,被认为是活性酯.这些吡啶的单酰基酯衍生物与 5-Fura 类似物相结合,开发出了含有 5-Fura 降解抑制剂的新型抗肿瘤药物.其中,3-[3-(6-苯甲酰氧基-3-氰基-2-吡啶氧羰基)苯甲酰]-1-乙氧基甲基-5-氟尿嘧啶(bof-A2)(22B)最为有效,目前正在进行第二阶段后期临床试验.
Doi:10.1248/cpb.41.1498

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-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.

专利号:US-2008214827-A1
优先权日:2004-02-03
标 题:Synthesis of Cyanoimino-Benzoimidazoles
发明人：GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
权利人:EURO CELTIQUE SA
摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

专利号:US-9650407-B2
优先权日:2011-11-02
标 题 :Reprogramming of cellular adhesion
发明人：GARTNER ZEV JORDAN; SELDEN NICHOLAS SCOTT; TODHUNTER MICHAEL E; LIANG SAMANTHA ISABEL; WEBER ROBERT JOSEPH; JEE NOEL YOUNGHO; LIU JENNIFER S
权利人:UNIV CALIFORNIA
摘要:Disclosed are membrane-anchored polynucleotides, and compositions comprising the membrane-anchored polynucleotides. Also disclosed are the processes for the synthesis of these compounds, compositions comprising such compounds, and the use of such compounds and compositions in research and therapeutic applications.