biostudies-literatureZheng LNational Natural Science Foundation of China5080-5085https://www.ebi.ac.uk/biostudies/studies/S-EPMC8694552biostudies-literatureUnknown11(9)Herein, we describe two novel strategies for the synthesis of esters, as achieved under high-speed ball-milling (HSBM) conditions at room temperature. In the presence of I<sub>2</sub> and KH<sub>2</sub>PO<sub>2</sub>, the reactions afford the desired esterification derivatives in 45% to 91% yields within 20 min of grinding. Meanwhile, using KI and P(OEt)<sub>3</sub>, esterification products can be obtained in 24% to 85% yields after 60 min of grinding. In addition, the I<sub>2</sub>/KH<sub>2</sub>PO<sub>2</sub> protocol was successfully extended to the late-stage diversification of natural products showing the robustness of this useful approach. Further application of this method in the synthesis of inositol nicotinate was also discussed.RSC advancesMechanically induced solvent-free esterification method at room temperature.PMC869455221978270Dushkin AVPolyakov NZheng LSun CYu JXu WSu WfalseMechanically induced solvent-free esterification method at room temperature.Herein, we describe two novel strategies for the synthesis of esters, as achieved under high-speed ball-milling (HSBM) conditions at room temperature. In the presence of I<sub>2</sub> and KH<sub>2</sub>PO<sub>2</sub>, the reactions afford the desired esterification derivatives in 45% to 91% yields within 20 min of grinding. Meanwhile, using KI and P(OEt)<sub>3</sub>, esterification products can be obtained in 24% to 85% yields after 60 min of grinding. In addition, the I<sub>2</sub>/KH<sub>2</sub>PO<sub>2</sub> protocol was successfully extended to the late-stage diversification of natural products showing the robustness of this useful approach. Further application of this method in the synthesis of inositol nicotinate was also discussed.2021-01-01T00:00:00Z2021 Jan2025-04-04T19:57:59.608Z2025-04-04T19:57:59.608ZS-EPMC86945523542445410.1039/d0ra09437d