Deuterium labeling techniques are widely utilized as efficient tools to study the absorption,distribution,metabolism,and excretion(ADME)of pharmaceuticals.Moreover,deuterium‐labeled drugs are expected to prolong the ...Deuterium labeling techniques are widely utilized as efficient tools to study the absorption,distribution,metabolism,and excretion(ADME)of pharmaceuticals.Moreover,deuterium‐labeled drugs are expected to prolong the half‐life of drug metabolism,enhance the efficacy of drugs,close metabolic sites,and decrease side effects.Thus,there is a rising demand for the practical construction of deuterium‐labeled drugs and their intermediates under mild conditions.This paper timely provides an overview of the recent advances in both photo‐and electro‐catalytic mild and selective deuteration of fine chemicals and pharmaceuticals with low‐cost and sustainable deuterium source.Three types of deuteration strategies are discussed according to the deuteration mode,named deuterium atom transfer strategy,deuterium atom abstraction strategy and deuterated water splitting strategy respectively.The application scope and mechanistic insights are discussed comprehensively.Finally,the perspective on the challenges and future development trends for photo‐and electro‐catalytic deuteration strategies are also presented.展开更多
We describe a specific procedure for the synthesis of deuterium-labelled 2-（1-methylalkyl）succinate established via alkylation of diethyl malonate, Krapcho decarboxylation reaction with D20 and hydrolysis reaction. ...We describe a specific procedure for the synthesis of deuterium-labelled 2-（1-methylalkyl）succinate established via alkylation of diethyl malonate, Krapcho decarboxylation reaction with D20 and hydrolysis reaction. Two novel compounds, 2-[^2H]-2-ethylsuccinic acid and 2-[^2H]-2-（1-methylhep- tyl）succinic acid were prepared via this synthetic route and characterized by mass spectrometry and ^1H NMR. The results showed that the 2-（1-methylalkyl）succinic acids were deuterated at the β-position, which is considered as an important reaction centre in the anaerobic degradation of n-alkanes.展开更多
The hydroarylation reaction of terminal alkynes with arylboronic acids catalyzed by low(400 ppm) loadings of palladium has been developed. The reaction is broad in scope and high-yielding, even on multigram scale. It ...The hydroarylation reaction of terminal alkynes with arylboronic acids catalyzed by low(400 ppm) loadings of palladium has been developed. The reaction is broad in scope and high-yielding, even on multigram scale. It is suitable for the synthesis of alkenes labeled with deuterium, and for the late-stage modification of bioactive molecules.展开更多
文摘Deuterium labeling techniques are widely utilized as efficient tools to study the absorption,distribution,metabolism,and excretion(ADME)of pharmaceuticals.Moreover,deuterium‐labeled drugs are expected to prolong the half‐life of drug metabolism,enhance the efficacy of drugs,close metabolic sites,and decrease side effects.Thus,there is a rising demand for the practical construction of deuterium‐labeled drugs and their intermediates under mild conditions.This paper timely provides an overview of the recent advances in both photo‐and electro‐catalytic mild and selective deuteration of fine chemicals and pharmaceuticals with low‐cost and sustainable deuterium source.Three types of deuteration strategies are discussed according to the deuteration mode,named deuterium atom transfer strategy,deuterium atom abstraction strategy and deuterated water splitting strategy respectively.The application scope and mechanistic insights are discussed comprehensively.Finally,the perspective on the challenges and future development trends for photo‐and electro‐catalytic deuteration strategies are also presented.
基金supported by the National Natural Science Foundation of China(No.41373070,51174092)the National Natural Science Foundation of China/Research Grants Council Joint Research Fund(No.41161160560)
文摘We describe a specific procedure for the synthesis of deuterium-labelled 2-（1-methylalkyl）succinate established via alkylation of diethyl malonate, Krapcho decarboxylation reaction with D20 and hydrolysis reaction. Two novel compounds, 2-[^2H]-2-ethylsuccinic acid and 2-[^2H]-2-（1-methylhep- tyl）succinic acid were prepared via this synthetic route and characterized by mass spectrometry and ^1H NMR. The results showed that the 2-（1-methylalkyl）succinic acids were deuterated at the β-position, which is considered as an important reaction centre in the anaerobic degradation of n-alkanes.
基金financial support from the National Natural Science Foundation of China (No. 21472033)the National Key R&D Program of China (No. 2018YFB1501604)the Fundamental Research Funds for the Central Universities (No. PA2020GDKC0021)。
文摘The hydroarylation reaction of terminal alkynes with arylboronic acids catalyzed by low(400 ppm) loadings of palladium has been developed. The reaction is broad in scope and high-yielding, even on multigram scale. It is suitable for the synthesis of alkenes labeled with deuterium, and for the late-stage modification of bioactive molecules.
