通过钯（II）催化的C(sp(3))-H偶联实现饱和氮杂环和N-甲基胺的α-芳基化反应
α-Arylation of Saturated Azacycles and N-Methylamines via Palladium(II)-Catalyzed C(sp(3))-H Coupling.
作者信息
Spangler Jillian E, Kobayashi Yoshihisa, Verma Pritha, Wang Dong-Hui, Yu Jin-Quan
机构信息
Department of Chemistry, The Scripps Research Institute , 10550 North Torrey Pines Road, La Jolla, California 92037, United States.
Medicinal Chemistry, Eisai Product Creation Systems, Eisai Co., Ltd. , 5-1-3 Tokodai, Tsukuba-shi, Ibaraki 300-2635, Japan.
出版信息
J Am Chem Soc. 2015 Sep 23;137(37):11876-9. doi: 10.1021/jacs.5b06740. Epub 2015 Sep 10.
Abstract
Pd(II)-catalyzed α-C(sp(3))-H arylation of pyrrolidines, piperidines, azepanes, and N-methylamines with arylboronic acids has been developed for the first time. This transformation is applicable to wide arrays of pyrrolidines and boronic acids, including heteroaromatic boronic acids. A diastereoselective one-pot heterodiarylation of pyrrolidines has also been achieved.
摘要
首次开发了钯（II）催化的吡咯烷、哌啶、氮杂环庚烷和N-甲胺与芳基硼酸的α-C(sp(3))-H芳基化反应。这种转化适用于多种吡咯烷和硼酸，包括杂芳基硼酸。还实现了吡咯烷的非对映选择性一锅法杂二芳基化反应。
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