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 113808-86-9 as follows. Computed Properties of C6H8N2O2
Example 139: 5-[4-(3,5-Dimethyl-1 H-pyrazole-4-carbonyl)-piperazin-1 -ylmethyl]- thiophene-2-carboxylic acid (2-methoxy-pyridin-4-ylmethyl)-amide trifluoroacetate To a solution of 3,5-dimethyl-1 H-pyrazole-4-carboxylic acid (18 mg, 0.13 mmol), HOBt*H2O (0.13 mmol), N-Methylmorpholine (1 mmol), 4-Dimethylaminopyridine (0.01 mmol) in 0.75 ml_ of DMF, a solution of intermediate 5 (0.1 1 mmol in 1 ml_ DMF) was added followed by EDC (neat, 0.13 mmol). The tube was closed with a screw cap and shaken over night at 40 C. 0.1 ml TFA was added and the volume was adjusted to 2.2 ml with DMF. The solution was filtered and submitted to preparative RP-HPLC purification to give 5-[4-(3,5-Dimethyl-1 H-pyrazole-4-carbonyl)-piperazin-1 -ylmethyl]- thiophene-2-carboxylic acid (2-methoxy-pyridin-4-ylmethyl)-amide trifluoroacetate as a colorless film (33 mg, 52%). 1 H NMR (DMSO-d6, 500 MHz) d ppm 9.22 (t, 1 H), 8.1 (d, 1 H), 7.80 (d, 1 H), 7.30 (bs, 1 H), 6.90 (d, 1 H), 6.69 (s, 1 H), 4.6 (bs, 2H), 4.40 (bs, 2H), 4.3-3.7 (broad signal, 4H), 3.7 (s, 3H), 3.5-3.0 (broad signal, 4H), 2.13 (s, 6H). LC/MS (Method 3); Rt = 1 .15 min; detected mass: m/z = 469.31 ([M+H]+)
According to the analysis of related databases, 113808-86-9, the application of this compound in the production field has become more and more popular.
Reference:
Patent; SANOFI; MENDEZ-PEREZ, Maria; BREITSCHOPF, Kristin; LORENZ, Katrin; STROBEL, Hartmut; WANG, Li-hsing; SCHIFFER, Alexander; GOERLITZER, Jochen; WO2015/82474; (2015); A1;,
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