"On Water" 直接 C-3 芳基化 2H-吡唑并[3,4-b]吡啶。
"On Water" Direct C-3 Arylation of 2H-Pyrazolo[3,4-b]pyridines.
机构信息
Euromed Faculty of Engineering, Euromed University of Fes (UEMF) , Route de Meknès, 30000 Fès, Morocco.
Institut de Chimie Organique et Analytique (ICOA), Université d'Orléans, UMR CNRS , 7311 BP 6759, 45067 Orléans Cedex 2, France.
出版信息
J Org Chem. 2017 Dec 1;82(23):12300-12306. doi: 10.1021/acs.joc.7b02136. Epub 2017 Nov 13.
An "on water" palladium-catalyzed direct (hetero)arylation of 2H-pyrazolo[3,4-b]pyridines has been developed. The reactions proceeds smoothly with at low catalytic loading at low temperature providing the C3 (hetero)arylated products in good to excellent isolated yields. Free NH 3-arylated 7-azaindazoles were also prepared by simple cleavage of the N-protected groups.
发展了一种"在水相"条件下钯催化的 2H-吡唑并[3,4-b]吡啶的直接（杂）芳基化反应。该反应在低温下以低催化负载量顺利进行，以良好至优异的分离收率得到了 C3（杂）芳基化产物。通过简单脱除 N-保护基，还制备了游离的 NH3-芳基化 7-氮杂吲哚。
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