CAS: 66607-27-0; 3-Iodo-1H-Indazole

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CAS号271-44-3 吲唑 | CAS号679794-95-7 3-trimethylsily... | CAS号40598-94-5 3-溴吲唑 | CAS号2596-89-6 3H-Indazol-3-im... | CAS号7647-01-0 盐酸 | CAS号43120-28-1 1H-吲唑-3-羧酸甲酯 | CAS号214541-51-2 3-(3-吲唑)丙酸 | CAS号205643-28-3 1-苄基-3-碘-1H-吲唑 | CAS号6814-68-2 3-乙基胺吲唑 | CAS号52088-10-5 3-碘-1-甲基-1H-吲唑 | CAS号49572-64-7 3-碘-2-甲基-2H-吲唑 | CAS号170632-47-0 利非西呱 | CAS号290368-00-2 N-(叔丁氧羰基)-3-碘吲唑 | CAS号65452-73-5 3-(4-methylphen... | CAS号918440-06-9 2-[(3-iodoindaz...

2-Methylbenzene Diazonium置于碘,Potassium Acetate,Potassium Hydroxide体系中,用 氯仿,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 8.0H,反应生成 3-碘吲唑
参考文献:Identification Of Novel Inhibitors Of Aurora A With A 3-(Pyrrolopyridin-2-yl)Indazole Scaffold
标题:Identification Of Novel Inhibitors Of Aurora A With A 3-(Pyrrolopyridin-2-yl)Indazole Scaffold
摘要:A Novel Series Of 3-(Pyrrolopyridin-2-yl)Indazole Derivatives Were Synthesized And Biologically Evaluated For Their Anti-Proliferative Effects On Five Human Cancer Cell Lines. As A Result,All Of Them Exhibited Vigorous Potency Against Hl60 Cell Line With Ic50 Values Ranging From Singe Digital Nanomolar To Micromolar Level. Besides,A Majority Of Them Displayed Modest To Good Antiproliferative Activities Against The Other Four Cell Lines,Including Kb,Smmc-7721,Hct116,And A549. Particularly,Compound 2Y,As The Most Distinguished One In This Series,Demonstrated Ic50 Values Of 8.3 Nm And 1.3 Nm Against Hl60 And Hct116 Cell Lines,Respectively. Afterwards,For Exploring The Molecular Target,Compounds 2D,2G And 2Y Were Further Selected To Evaluate The Inhibitory Activities Against A Panel Of Kinases. Finally,They Were Identified To Be Targeting Aurora A Kinase With Significant Selectivity Over Other Kinases,Such As Chk1,Cdk2,Mek1,Gsk3 Beta,Braf,Ikk Beta And Pkc. (C) 2015 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Bmc.2015.02.004

专利信息

专利号:US-2006116519-A1
优先权日:2004-11-17
标 题:Synthesis of 5-bromo-4-methyl-pyridin-3-ylmethyl)-ethyl-carbamic acid tert-butyl ester
发明人：MA CHUNRONG; TIAN QINGPING
权利人:AGOURON PHARMA
摘要:The present invention relates to novel synthetic methods for the preparation of intermediates of 3{5-[3-(4,6-Difluoro-1H-benzoimidazol-2-yl)-1H-indazol-5-yl]4-methyl-pyridin-3-yl methyl}-ethyl-amine.

专利号:WO-2015131100-A1
优先权日:2014-02-28
标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids
发明人：YU JIN-QUAN
权利人:SCRIPPS RESEARCH INST
摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.

专利号:WO-2008022467-A1
优先权日:2006-08-25
标 题 :2-substituted azain doles and 2 substituted thienopyrroles, their precursors and novel processes for the preparation thereof
发明人：LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING
权利人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING
摘要:The present invention relates generally to processes for the chemical synthesis of azaindole and thienopyrrole compounds, in particular azaindole and thienopyrrole compounds that are substituted at the 2-position of the azaindole or thienopyrrole ring, and optionally at additional locations of the azaindole or thienopyrrole ring such as the 1- and/or 3-position, compounds prepared by such processes, and synthetic precursors of such processes. More particularly, the present invention relates to the preparation of 2- substituted azaindoles from an ortho-gem-dihalovinylaminopyridine or from an ortho- gem-dihalovinylaminopyridine N-oxide compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to the preparation of 2-substituted thienopyrroles from an ortho-gem-dihalovinylthiophene compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to processes for the production of ortho-gem- dihalovinylaminopyridines which are useful as starting materials in the production of 2- substituted azaindoles, and novel compounds prepared by the processes. The present invention also relates to processes for the production of ortho-gem-dihalovinylthiophenes which are useful as starting materials in the production of 2-substituted thienopyrroles, and novel compounds prepared by the processes. Formulae (V) and (VII).

专利号:WO-2024193328-A1
优先权日:2023-03-20
标题 :Indazole substituted podophyllotoxin derivative, preparation method therefor, and use thereof
发明人：TANG YAJIE; ZHAO WEI; TANG YUNZHI
权利人:TANG YAJIE
摘要:An indazole nitrogen-substituted podophyllotoxin derivative represented by formula (V), a synthesis method therefor, and a use thereof. Different substituents, such as methyl, ethyl, propyl, benzyl, a fluorine atom, a chlorine atom, a bromine atom, an iodine atom, etc., are respectively introduced into the 1 and 3 positions of indazole podophyllotoxin to obtain a compound represented by formula (V) having significantly improved antitumor activity.