Introduction of a new synthetic route about 3-(Chloromethyl)-1H-1,2,4-triazol-5(4H)-one

According to the analysis of related databases, 252742-72-6, the application of this compound in the production field has become more and more popular.

In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 252742-72-6 as follows. 252742-72-6

Example 53 (3R*,4R*)-N-[3,5-bis(trifluoromethyl)benzyl]-3-(4-fluorophenyl)-N-methyl-1-[(5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl)methyl]piperidine-4-carboxamide hydrochloride To a solution of the compound (0.30 g) obtained in Example 11 and potassium carbonate (0.083 mg) in 1percent H2O-DMF (5.0 mL) was added 5-(chloromethyl)-2,4-dihydro-3H-1,2,4-triazol-3-one (0.096 g) at 0¡ãC, and the mixture was stirred at room temperature for 14 hr. The reaction mixture was poured into water, and the product was extracted with ethyl acetate. The organic layer was washed with brine and dried, and the solvent was evaporated under reduced pressure. The obtained residue was purified by preparative HPLC. The obtained product was treated with 1 equivalent of 4N hydrogen chloride/ethyl acetate solution to give the title compound as a white powder (0.30 g, 89percent). MS(ESI+): 560(M-HCl+H)

According to the analysis of related databases, 252742-72-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Takeda Pharmaceutical Company Limited; EP1705176; (2006); A1;,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics