With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.192130-34-0,tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
N-(5-tert-Butylisoxazol-3-yl)-N- {3- [ (2-chloropyrimidin-5-yl) ethynyl] phenyl} urea (Intermediate 9) (0.22 g) and tert-butyl 4-(2-aminoethyl)-piperazine-1-carboxylate (0.38 g) were stirred in MeCN (10 mL) and hydrogen chloride (I. OM solution in ether) (0.11 mL) was added dropwise. The reaction mixture was stirred and heated at 70¡ãC for 4 hours. The solvent was evaporated and the residue was dissolved in DCM (20 mL) and TFA (10 mL). The reaction mixture was stirred at ambient temperature for 2 hours, the solvent was evaporated and the product was purified by flash chromatography on silica using 1-20percent (7N NH3 in MeOH) in DCM as eluent. The product was triturated with ether to give the title compound as an off-white solid (274 mg, 99percent); ‘H NMR (DMSO-d6) 1.29 (s, 9H), 2.45-2. 57 (m, 2H), 2.57-2. 65 (m, 4H), 3.03-3. 10 (m, 4H), 3.39-3. 49 (m, 2H), 6.49 (s, 1H), 7.10-7. 16 (m, 1H), 7.29-7. 35 (m, 2H), 7.51 (t, 1H), 7.75 (s, 1H), 8.40-8. 52 (m, 3H), 8.99 (s, 1H), 9.62 (s, 1H) ; MS m/e MH+ 489.
192130-34-0, 192130-34-0 tert-Butyl 4-(2-aminoethyl)piperazine-1-carboxylate 1514400, apiperazines compound, is more and more widely used in various.
Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2005/60970; (2005); A1;,
Piperazine – Wikipedia
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