CAS: 779353-01-4; (S)-3-(((3-Ethyl-5-(2-(2-Hydroxyethyl)Piperidin-1-yl)Pyrazolo[1,5-A]Pyrimidin-7-yl)Amino)Methyl)Pyridine 1-Oxide

上下游产品

5-chloro-3-ethyl-N-[(1-oxido-pyridinyl)methyl]pyrazolo-[1,5-a]pyrimidine-5.7(4H,6H)-dion-7-amine (2S)-2-(2-methoxyethyl)piperidine

(S)-(-)-2-哌啶乙醇,3-(((5-氯-3-乙基吡唑并[1,5-A]嘧啶-7-基)氨基)甲基)吡啶1-氧化物置于sodium Carbonate体系中,用 N-甲基吡咯烷酮,水 作为反应溶剂,化学反应 12.0H,反应生成 (2S)-1-[3-乙基-7-[[(1-氧代-3-吡啶基)甲基]氨基]吡唑并[1,5-A]嘧啶-5-基]-2-哌啶乙醇
参考文献:Process And Intermediates For The Synthesis Of (3-Alkyl-5-Piperidin-1-Yl-3,3A-Dihydro-Pyrazolo[1,5-A]Pyrimidin-7-yl)-Amino Derivatives And Intermediates
标题:Process And Intermediates For The Synthesis Of (3-Alkyl-5-Piperidin-1-Yl-3,3A-Dihydro-Pyrazolo[1,5-A]Pyrimidin-7-yl)-Amino Derivatives And Intermediates
摘要:该申请公开了一种合成(3-烷基-5-哌啶-1-基-3,3A-二氢-吡唑啉[1,5-A]嘧啶-7-基)-氨基衍生物的新工艺,以及在合成过程中有用的中间体.所述(3-烷基-5-哌啶-1-基-3,3A-二氢-吡唑啉[1,5-A]嘧啶-7-基)-氨基衍生物在制药制剂中作为细胞周期蛋白依赖激酶抑制剂化合物(cdk抑制剂)具有用途.

专利信息

专利号:US-8076479-B2
优先权日:2006-08-28
标题 :Process and intermediates for the synthesis of (3-alkyl-5-piperidin-1-yl-3,3a-dihydro-pyrazolo[1,5-a]pyrimidin-7-yl)-amino derivatives and intermediates
发明人：CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI
权利人:CHEN FRANK XING; KEERTIKAR KARTIK M; KUO SHEN-CHUN; LEE HONG-CHANG; RAGHAVAN RAMANI R; WU GEORGE G; XIE JI; SCHERING CORP
摘要:Disclosed is a process for the synthesis of compounds of Formula I n nby sequentially aminating, first with a primary amine and then with a secondary amine, an intermediate compound of the structure of Formula E1,n n nwherein R 1 is a linear, branched, or cyclic alkyloxy functional group of the structure (—R 2a —OH), R 2a is a linear, branched or cyclic alkyl group, R 2 is a linear, branched or cyclic alkyl group, and R 3 is an alkylene-heterocycle, said process comprising forming intermediate compound of Formula E1 by reacting, in a refluxing reaction solvent selected from alcohols having 5 or less carbon atoms and mixtures of two or more thereof, a methanol solution of a salt of a 4-alkyl-3-amino-pyrazole compound of Formula C1,n n nwith a diamidization reagent selected from dimethylmalonate, monomethylmalonyl-chloride, and malonyl dichloride in the presence of a Lewis base having sufficient proton affinity to abstract a proton from the 1-position nitrogen on the pyrazole ring.

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-12043612-B2
优先权日:2020-05-09
标 题 :Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same
发明人：ALLAN LAURA E N; CHEN CHUNGPIN HERMAN; DONG HANQING; GROSSO JOHN A; HASKELL III ROYAL J; LLOYD RHYS; REECE HAYLEY
权利人:ARVINAS OPERATIONS INC
摘要:The present disclosure relates to ultra-pure forms, polymorphs, amorphous forms, and formulations of N-[(1r,4r)-4-(3-chloro-4-cyanophenoxy)cyclohexyl]-6-[4-({4-[2-(2,6-dioxopiperidin-3-yl)-6-fluoro-1,3-dioxo-2,3-dihydro-1H-isoindol-5-yl]piperazin-1-yl}methyl)piperidin-1-yl]pyridazine-3-carboxamide, referred to herein as Compound A:The present disclosure also relates methods of manufacturing and purifying the same, as well as intermediates useful in the synthesis of Compound A. The ultra-pure forms, polymorphs, amorphous forms, and formulations of Compound A can be used as therapeutic agents for the treatment of various diseases and conditions such as cancer.

专利号:US-7786306-B2
优先权日:2006-08-18
标 题 :Process for resolving chiral piperidine alcohol and process for synthesis of pyrazolo[1,5-a] pyrimidine derivatives using same
发明人：CHEN FRANK XING; TAMAREZ MARIA M; XIE JI
权利人:SCHERING CORP
摘要:The present invention provides a method of resolving piperdin-yl-alkylene-alcohols, in high yield at high enantiomeric purity, for example 2-piperidin-2-yl-ethanol.

专利号:US-2018371021-A1
优先权日:2017-05-11
标 题 :Peptidomimetic macrocycles and uses thereof
发明人：AIVADO MANUEL; GUERLAVAIS VINCENT; OLSON KAREN
权利人:AILERON THERAPEUTICS INC
摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.