The Ritter-type reaction, without relying on a pre-installed functional group, is a highly efficient tool forthe construction of amides. However, the intrinsic chemo-selectivity that determines the generation ofamides...The Ritter-type reaction, without relying on a pre-installed functional group, is a highly efficient tool forthe construction of amides. However, the intrinsic chemo-selectivity that determines the generation ofamides or byproducts limits the efficiency and yield of the reaction. From 68 different types of hydrates,we found that a coordinatively unsaturated inorganic salt hydrate, MgSO_(4)·2H_(2)O, controlled chemoselectivity and eliminated the shortcomings of other synthesis approaches. To rationalize the differencesin selectivity of inorganic salt hydrates, we analyzed their corresponding water content, alkalinity, anions,and cations. MgSO_(4)·2H_(2)O was used with diverse scaffolds and C–H oxygenations, which demonstratedits generality in synthetic utility. Because it is readily available and it significantly improves yield, we expectthat MgSO_(4)·2H_(2)O will have broad application for Ritter-type reactions.展开更多
基金support from the Research Foundation for Talented Scholars of Fujian Medical University(grant number:XRCZX2018014)the Joint Funds for the Innovation of Science and Technology,Fujian province(grant number:2018Y9072)the Natural Science Foundation of Fujian Province,China(grant number:2021J01693).
文摘The Ritter-type reaction, without relying on a pre-installed functional group, is a highly efficient tool forthe construction of amides. However, the intrinsic chemo-selectivity that determines the generation ofamides or byproducts limits the efficiency and yield of the reaction. From 68 different types of hydrates,we found that a coordinatively unsaturated inorganic salt hydrate, MgSO_(4)·2H_(2)O, controlled chemoselectivity and eliminated the shortcomings of other synthesis approaches. To rationalize the differencesin selectivity of inorganic salt hydrates, we analyzed their corresponding water content, alkalinity, anions,and cations. MgSO_(4)·2H_(2)O was used with diverse scaffolds and C–H oxygenations, which demonstratedits generality in synthetic utility. Because it is readily available and it significantly improves yield, we expectthat MgSO_(4)·2H_(2)O will have broad application for Ritter-type reactions.
