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

• 来源期刊: 科学通报（英文版）
• 年，卷（期）: 2019,（11）
• 页码范围: 723-729
• 页数: 7页
• 语种: 英文

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.