Feedstocks to Pharmacophores: Cu-Catalyzed Oxidative Arylation of Inexpensive Alkylarenes Enabling Direct Access to Diarylalkanes.
Feedstocks to Pharmacophores: Cu-Catalyzed Oxidative Arylation of Inexpensive Alkylarenes Enabling Direct Access to Diarylalkanes.
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药效基团原料：铜催化廉价烷基芳基化，能够直接获得二芳基烷烃。
DOI：
10.1021/jacs.7b03387
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发表时间：
2017
影响因子：
15
通讯作者：
Stahl,ShannonS
中科院分区：
文献类型：
--
作者：
Vasilopoulos,Aristidis;Zultanski,SusanL;Stahl,ShannonS
一种铜催化的方法已经确定了选择性氧化芳基硼酯的苯基C-H键。所得到的1,1-二芳烷可以直接从含有伯和仲苯基C-H键的廉价烷基烯（如甲苯或乙苯）中得到。所有的催化剂成分都是低成本的，芳基硼酯要么是市售的，要么是很容易从市售的硼酸中获得的。强调了这些方法在药物化学应用中的潜在效用。
A Cu-catalyzed method has been identified for selective oxidative arylation of benzylic C–H bonds with arylboronic esters. The resulting 1,1-diarylalkanes are accessed directly from inexpensive alkylarenes containing primary and secondary benzylic C–H bonds, such as toluene or ethylbenzene. All catalyst components are commercially available at low cost, and the arylboronic esters are either commercially available or easily accessible from the commercially available boronic acids. The potential utility of these methods in medicinal chemistry applications is highlighted.