With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.304897-49-2,tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
2,4-Dichloro-5-(trifluoromethyl)pyrimidine (0.546 g, 2.52 mmol) in 1 : 1 dichioroethane: fe/f-butanol was cooled to 0 C under nitrogen. A 1.0 M solution of zinc(ll) chloride in diethyl ether (3.43 mL, 3.34 mmol) was added, and the mixture stirred for one hour at 0 C. iert-Butyl 4-(4-aminobenzyi)piperazine-1-carboxylate (193) (0.667 g, 2.29 mmol) in 1 : 1 dichioroethane: ferf-butanol (20 mL) vv’as added dropwise over thirty minutes, followed by triethyiamine (0.351 mL, 2.52 mmol) in 1 :1 dichioroethane: ferf-butanol (10 mL). The mixture was stirred overnight, allowing the ice bath to come to room temperature over this time. The mixture was concentrated onto silica gel and chromatographed (40 g silica cartridge, 0-100% ethyl acetate/petroleum benzine 40- 60 C) to give a residue which was triturated with petroleum benzine 40-60 C to give the title compound {194) (0.976 g, 90%) as an off white solid; 1H NMR (400 MHz, dr MeOD) delta 8.68 (d, J = 0.6 Hz, 1 H), 7.85 (d, J = 8.6 Hz, 2H), 7.51 (d, J = 8.6 Hz, 2H), 4.30 (s, 2H), 3.27 – 3,00 (br, overlaps with solvent), 1.47 (s, 9H). LCMS Method C: 5.08 min; m/z 472.1 [M+H]+; m/z 470.1 [M-H]
304897-49-2, 304897-49-2 tert-Butyl 4-(4-aminobenzyl)piperazine-1-carboxylate 12045001, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; CANCER THERAPEUTICS CRC PTY LTD; DEVLIN, Mark Graeme; STREET, Ian Philip; TONG, Warwick Bonner; WO2014/27199; (2014); A1;,
Piperazine – Wikipedia
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