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Mechanically induced solvent-free esterification method at room temperature.


ABSTRACT: 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 I2 and KH2PO2, the reactions afford the desired esterification derivatives in 45% to 91% yields within 20 min of grinding. Meanwhile, using KI and P(OEt)3, esterification products can be obtained in 24% to 85% yields after 60 min of grinding. In addition, the I2/KH2PO2 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.

SUBMITTER: Zheng L 

PROVIDER: S-EPMC8694552 | biostudies-literature | 2021 Jan

REPOSITORIES: biostudies-literature

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Mechanically induced solvent-free esterification method at room temperature.

Zheng Lei L   Sun Chen C   Xu Wenhao W   Dushkin Alexandr V AV   Polyakov Nikolay N   Su Weike W   Yu Jingbo J  

RSC advances 20210128 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</su  ...[more]

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