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1-(4-methylbenzoyl)pyrrolidine synthesis

8synthesis methods
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Yield:59746-40-6 96%

Reaction Conditions:

Stage #1: 4-methylbenzoic acidwith N-((2,2-dimethyl-1,3-dioxolan-4-yl)methyl)-N-ethynylmethanesulfonamide in dichloromethane at 20;
Stage #2: tetrahydropyrrole in dichloromethane;

Steps:

3

Take methyl benzoic acid (0.5mmol),N-(2,2-Dimethyl-1,3-dioxolane-4-ylmethyl)-N-ethynylmethanesulfonamide (0.55mmol) was dissolved in 3mL of dichloromethane,Stir the reaction at room temperature,TLC monitors the reaction process, and when the raw material acid is consumed completely,Add tetrahydropyrrole (0.55mmol),TLC monitors the reaction process,After the reaction, the solvent was distilled off under reduced pressure,Add a small amount of ethanol,Add 10mL of 0.5M dilute hydrochloric acid,After stirring for 10 min, the product precipitated out,Filter and wash, collect solids,The pure product was obtained as a white solid with a yield of 96%.The following are the structural formula and nuclear magnetic resonance experimental data of the product,Mass spectrometry experiment data:

References:

CN112341423,2021,A Location in patent:Paragraph 0153-0158