630125-91-6,With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.630125-91-6,4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline,as a common compound, the synthetic route is as follows.
To a suspension of triphosgene (0.21 g, 0.71 mmol) and Na2C03 (0.45 g, 4.27 mmol) in DCM (18 ml), kept at 0 ocunder argon, 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (0.61 g, 2.13 mmol) was added. Thereaction was monitored by HPLC (following the formation of 4-ethyl-piperazine-1-carboxylic acid [4-(4-ethylpiperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-amide by treating a sample of the reaction mixture with N-25 ethylpiperazine). After 1 h, 3-ethynyl-phenylamine (0.26 g, 2.18 mmol) was added and the reaction was let understirring overnight at r.t.. The mixture was diluted with DCM, washed with water (3 x 10 ml), dried over anhydrousNa2S04 and concentrated under vacuum. Purification by flash column chromatography (DCM/MeOH 95/5) affordedthe product as yellow solid (0.64 g, 70%).1H NMR (600 MHz, DMSO-dG) o ppm 0.95-1.00 (m, 3 H) 2.22-2.47 (m, 10 H) 3.52 (s, 2 H) 4.14 (s, 1 H) 7.09 (d,30 J=7.69 Hz, 1 H) 7.30 (t, J=7.88 Hz, 1 H) 7.41 (dd, J=8.24, 1.28 Hz, 1 H) 7.56 (dd, J=8.61, 1.83 Hz, 1 H) 7.61 – 7.64(m, 1 H) 7.66 (t, J=1.65 Hz, 1 H) 7.95 (d, J=2.01 Hz, 1 H) 8.85 (s, 1 H) 9.02 (s, 1 H).
As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.
Reference：
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; MENICHINCHERI, Maria; ANGIOLINI, Mauro; BERTRAND, Jay Aaron; CARUSO, Michele; POLUCCI, Paolo; QUARTIERI, Francesca; SALOM, Barbara; SALSA, Matteo; ZUCCOTTO, Fabio; WO2014/72220; (2014); A1;,
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