论文摘要
With the growing urgency of potential catastrophic climate changes due to anthropogenic CO2 emissions,numerous efforts have been devoted to development of synthetic protocols using CO2 as a building block in organic reactions, but the general applicability to complex drug-like substrates remains a challenge.We develop a general protocol for scalable direct N-methylation of a wide-scope drug-like amines using CO2 and polymethylhydrosiloxane—a nontoxic, aerobically-stable hydrosilane considered as an industrial waste—via simple inorganic base catalysis. A rare application of the Sabatier principle in organic chemistry led to the discovery of cheap, nontoxic K3PO4 as an efficient catalyst. Preparations of a wide-scope drug-like amines with carbon-isotope label were also successfully achieved, enabling direct use of CO2 in studies of drug absorption, distribution, metabolism and excretion.
论文目录
文章来源
类型: 期刊论文
作者: Chunlei Lu,Zetian Qiu,Yiling Zhu,Bo-Lin Lin
来源: Science Bulletin 2019年11期
年度: 2019
分类: 基础科学,工程科技Ⅰ辑
专业: 化学
单位: School of Physical Science and Technology (SPST), ShanghaiTech University,Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences,University of Chinese Academy of Sciences
基金: supported by the National Natural Science Foundation of China(U1532135)
分类号: O643.32
页码: 723-729
总页数: 7
文件大小: 837K
下载量: 3
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