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• Preparation

  Teneligliptin was synthesized from N-Boc piperazine and diketene via condensation, cyclization, and deprotection to obtain intermediate 1-(3-methyl-1-phenyl-1H-pyrazole-5-yl)piperazine; then, using trans-4-hydroxy-L-proline as a starting material, it underwent Fmoc protection, oxidation, and condensation to obtain intermediate 3-[(2S)-1-(9H-fluorene-9-ylmethoxycarbonyl)-4-oxopyrrolidine-2-ylcarbonyl]thiazolidin; finally, these two intermediates were reductively aminationed and deprotected to obtain the antidiabetic drug Teneligliptin, with an overall yield of 47.2% (based on trans-4-hydroxy-L-proline) and a purity of 99.1% (HPLC). The structure of Teneligliptin was confirmed by MS, IR, 1H-NMR, and 13C-NMR spectra. This synthetic route utilizes inexpensive and readily available raw materials, mild reaction conditions, simple post-processing, and high yield, laying the foundation for pilot-scale production.;

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