CAS: 55919-82-9; 5-Iodo-1H-Indazole

上下游产品

5-氨基吲唑 1H-Indazol-5-Ylamine 19335-11-6
5-溴吲唑 5-Bromo-1H-Indazole 53857-57-1

5-溴吲唑置于trans-N,N'-Dimethyl-1,2-Cyclohexyldiamine,Copper(L) Iodide Sodium Iodide体系中,用 1,4-二氧六环 作为反应溶剂,化学反应 68.0H,以100%的收率获得产物5-碘-1H-吲唑
参考文献:Wo2008/116833
标题:Wo2008/116833

专利信息

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.