Preparation method of trifluoroethyl-containing azetidine derivative

The invention discloses a preparation method of a trifluoroethyl-containing azetidine derivative, which comprises the following steps: mixing alkyne amine with a structure as shown in a formula II, 1-(trifluoromethyl)-1, 2-benzioyl-3 (1H)-ketone with a structure as shown in a formula III, 10-methyl-...

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Hauptverfasser: LUO FANG, BAI YIHUI, ZHU GANGGUO, ZHOU GENLAI, SHANG TIANBO
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention discloses a preparation method of a trifluoroethyl-containing azetidine derivative, which comprises the following steps: mixing alkyne amine with a structure as shown in a formula II, 1-(trifluoromethyl)-1, 2-benzioyl-3 (1H)-ketone with a structure as shown in a formula III, 10-methyl-9-mesitylene acridine perchlorate with a structure as shown in a formula IV and cesium carbonate in a solvent, and reacting to obtain the trifluoroethyl-containing azetidine derivative. According to the invention, a photocatalytic trifluoromethylation/cyclization cascade reaction strategy is adopted, and stereoselective synthesis of the derivative containing trifluoroethyl azetidine is realized in one step. The reaction conditions are mild, the substrate application range is wide, structural diversity synthesis of the preparation method of the trifluoroethyl-containing azetidine derivative can be realized by changing substituent groups, the reaction yield is good, the operation is simple, and a new way is provided