Application of 143879-78-1, 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 143879-78-1 as follows.
Methyl 1 -methyl-4-[ [(1 S)-2,2,2-trifluoro- i-methyl-ethyl] sulfamoyl]pyrrole-2-carboxylate (0.7 g, 2.23 mmol) was dissolved in THF (10 mL) under nitrogen. To this was added 3-amino-2,6- difluorobenzonitrile (0.45 g, 2.9 mmol) and the mixture was cooled in an ice-water bath while stirred under nitrogen. To this was added drop wise lithium bis(trimethylsilyl)amide 1M intoluene (6.68 mL, 6.68 mmol) over a period of 10 minutes. The resulting mixture was stirred for1 hour while cooling was continued. The mixture was quenched with saturated ammonium chloride (25 mL) and the resulting mixture was extracted using EtOAc (3 x 25 mL). The combined extracts were washed with brine (20 mL), dried on Na2SO4, filtered and concentrated in vacuo. The obtained residue was dissolved in 2 mL dichloromethane and this was loaded on a dry silica plug. This was purified by column chromatography using gradient elution fromheptane to EtOAc. (100:0 to 0:100). The desired fractions were collected and concentrated in vacuo yielding a powder. This powder was recrystallized out of MeOH/water. The obtained crystals were collected on a filter, rinsed with water followed by diisopropylether and dried in a vacuo at 55C for 24 hours resulting in N-(3-Cyano-2,4-difluorophenyl)-1-methyl-4-{[(1S)- 2,2,2-trifluoro- 1 -methylethyl] sulfamoyl} -1 H-pyrrole-2-carboxamide (563 mg) as a powder.Method A: Rt: 1.75 mm mlz: 435.0 (M-H) Exact mass: 436.06. ?H NMR (400 MHz, DMSO-d6) oe ppm 1.09 (d, J=6.8 Hz, 3 H), 3.80 – 4.06 (m, 4 H), 7.36 (d, J2.0 Hz, 1 H), 7.40 – 7.51 (m, 1 H), 7.66 (d, J=1.5 Hz, 1 H), 7.85 – 8.02 (m, 1 H), 8.54 (br. s, 1 H), 10.14 (br. s, 1 H).
According to the analysis of related databases, 143879-78-1, the application of this compound in the production field has become more and more popular.