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Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof
Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof
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机译:通过催化C-H活化/硼化/胺化反应由芳烃合成氨基芳基硼酸酯和取代苯胺及其用途
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摘要
A process is described for synthesizing aminoarylboronic esters of the general formula chemistry chemdraw filechemistry mol file;wherein R, R2, and R3 are each an alkyl, aryl, vinyl, alkoxy, carboxylic esters, amides, or halogen; Ar is any variety of phenyl, naphthyl, anthracyl, heteroaryl; and R1 is alkyl, hydrogen, or aryl. The aminoarylboronic esters are produced via the metal-catalyzed coupling of arylboronic esters of the general formula chemistry chemdraw filechemistry mol file;wherein R and R1 are any non-interfering group and X is chloro, bromo, iodo, triflates, or nonaflates to amines (primary and secondary). In particular, a process is described for the synthesis of the aminoarylboronic esters via a step-wise or tandem process in which one catalytic event is a metal-catalyzed borylation and the other catalytic event is a metal-catalyzed amination.
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机译:描述了一种合成通式的氨基芳基硼酸酯的方法 <图像文件=“ US20040024237A1-20040205-C00001.GIF” he =“ 51.11505” id =“ EMI-C00001” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 48.96045“ /> 化学化学绘图文件 ExternalFileRef> 化学mol文件 ExternalFileRef> Chemistry>;其中R,R 2 Sub>和R 3 Sub>分别为烷基,芳基,乙烯基,烷氧基,羧基酯,酰胺或卤素; Ar是任何种类的苯基,萘基,蒽基,杂芳基; R 1 Sub>是烷基,氢或芳基。氨基芳基硼酸酯是通过金属催化的通式为芳基硼酸酯的偶合生成的 <图像文件=“ US20040024237A1-20040205-C00002.GIF” he =“ 23.27535” id =“ EMI-C00002” imgContent =“ undefined” imgFormat =“ GIF” wi =“ 41.0508“ /> 化学化学绘图文件 ExternalFileRef> 化学mol文件 ExternalFileRef> Chemistry>;其中R和R 1 Sub>是任何非干扰基团,X是氯,溴,碘,三氟甲磺酸酯或对氨基的非aflates(伯和中学)。特别地,描述了通过逐步或串联方法合成氨基芳基硼酸酯的方法,其中一个催化事件是金属催化的硼化,而另一催化事件是金属催化的胺化。
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