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 solution of 100 mg (0.69 mmol) of 3-ethynyl benzoic acid in 5 mL of dry N,N-dimethylformamide, 164 mg (0.57 mmol) of 4-[(4-ethylpiperazin-1-yl)methyl]-3-(trifluoromethyl)aniline (prepared as described in J. Med. Chem., (2010) 53, 4701-4719) 242 mg (0.75 mmol) of TBTU and 0.14 mL (0.82 mmol) of DIPEA were added consecutively. After 15 h under stirring at room temperature the mixture was poured into aqueous NaHC03 and extracted twice with ethylacetate. The organic phase was then washed with brine, dried over Na2S04 and evaporated to dryness. A flash- chromatography on silica gel (DCM-MeOH-NH3 7N in methanol 9/1/0.04), afforded 149 mg of the title compound (63%). 1H NMR (600 MHz, DMSO-d6) delta ppm 0.99 (t, J=7.14 Hz, 3 H) 2.19 – 2.46 (m, 10 H) 3.57 (s, 3 H) 6.61 (br. s., 2 H) 7.60 (t, J=7.88 Hz, 1 H) 7.64 (d, J=2.20 Hz, 1 H) 7.72 (d, J=8.61 Hz, 1 H) 7.80 (dt, J=7.83, 1.21 Hz, 1 H) 7.91 – 7.98 (m, 1 H) 8.05 (dd, J=8.52, 1.92 Hz, 1 H) 8.12 (s, 1 H) 8.16 (t, J=1.47 Hz, 1 H) 8.21 (d, J=2.20 Hz, 1 H) 10.59 (s, 1 H) 12.08 (br. s., 1 H) HRMS (ESI) calcd for C29H28N7OF3 [M+H]+ 548.2380, found 548.2392.
As the paragraph descriping shows that 630125-91-6 is playing an increasingly important role.
Reference£º
Patent; NERVIANO MEDICAL SCIENCES S.R.L.; ANGIOLINI, Mauro; BUFFA, Laura; MENICHINCHERI, Maria; MOTTO, Ilaria; POLUCCI, Paolo; TRAQUANDI, Gabriella; ZUCCOTTO, Fabio; WO2014/184069; (2014); A1;,
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