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 (17.2 mg, 0.058 mmol) and Na2C03 (37 mg, 0.348 mmol) in DCM (2 ml), kept atooc under argon, 4-(4-ethyl-piperazin-1-ylmethyl)-3-trifluoromethyl-phenylamine (50 mg, 0.17 4 mmol) was added.The reaction was monitored by HPLC (following the formation of 4-ethyl-piperazine-1-carboxylic acid [4-(4-ethyl-5 piperazin-1-ylmethyl)-3-trifluoromethyl-phenyl]-amide by treating a sample of the reaction mixture with Nethylpiperazine).After 1 h a solution of 2-[2-amino-5-(3-amino-phenylethynyl)-pyrimidin-4-yl]-1-methyl-1 ,5,6, 7-tetrahydro-pyrrolo[3,2-c]pyridin-4-one (1 04 mg, 0.226 mmol) in DMA (1.5 ml) was added and the reaction was letunder stirring overnight. The mixture was diluted with DCM, washed with water (3 x 10 ml), dried over anhydrousNa2S04 and taken to dryness under vacuum. Purification by flash column chromatography (DCM/MeOH 95/5)10 afforded the product as yellow solid (70 mg, 52%).1H NMR (401 MHz, DMSO-dG) o ppm 0.97 (t, J=7.20 Hz, 3 H) 1.45 (s, 9 H) 2.23- 2.45 (m, 10 H) 3.00 (t, J=6.3 Hz, 2H) 3.51 (s, 2 H) 3.84 (s, 3 H) 4.00 (t, J=6.16 Hz, 2 H) 7.06 (d, J=7.69 Hz, 1 H) 7.11 (s, 2 H) 7.25-7.31 (m, 1 H) 7.43(d, J=8.06 Hz, 1 H) 7.49 (s, 1 H) 7.56- 7.65 (m, 2 H) 7.72 (t, J=1.71 Hz, 1 H) 8.01 (d, J=1.71 Hz, 1 H) 8.50 (s, 1 H),10.00 (bs, 1 H), 10.19 (bs, 1 H).
630125-91-6, 630125-91-6 4-((4-Ethylpiperazin-1-yl)methyl)-3-(trifluoromethyl)aniline 59134564, apiperazines compound, is more and more widely used in various fields.
Reference£º
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;,
Piperazine – Wikipedia
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