Scalable direct N-methylation of drug-like amines using 12CO2/13CO2 by simple inorganic base catalysis

Scalable direct N-methylation of drug-like amines using 12CO2/13CO2 by simple inorganic base catalysis

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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Scalable direct N-methylation of drug-like amines using 12CO2/13CO2 by simple inorganic base catalysis
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