With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.184637-48-7,tert-Butyl 3-aminopiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.
184637-48-7, To a solution of Intermediate 2 (1 g) in dry DMF (10 ml) under nitrogen was added (+/-)-3-amino-l-N-Boc-rhoiperidine (CAS 184637-48-7) (500 mg) and Na2CO3 (1.32 g). The mixture was heated at 110¡ãC for 24 hours, a further 250 mg of (+/-)-3-amino-l- N-Boc-piperidine was added and heating continued for another 24 hours. The mixture was cooled to r.t, concentrated in vacuo and the residue dissolved in MeOH (20 ml). To this was added KOEta (330 mg) and the mixture stirred at r.t. overnight. The solvent was removed in vacuo and the residue was extracted with EtOAc (200 ml). The organic layer was washed with water (50 ml), washed with brine (50 ml), separated, dried over MgSO4, filtered and the solvent removed in vacuo. Purification by column chromatography on silica eluting with 10-50percent EtO Ac/heptane afforded a solid, which was dissolved in DCM (75ml) and treated with 2N HCl in ether (5 ml) for 24 hours. The solvent was removed in vacuo and the resulting solid triturated in Et2O to afford the title compound as a yellow solid (585 mg, 58percent). LCMS 328/330 [M+Eta]+, RT 1.92 min. 1H NMR 300 MHz (d6- DMSO) 12.00 (1H, s, br), 9.15-8.85 (2H, d, br), 8.80-8.40 (2H, m), 8.35 (1H, s), 7.50 (2H, d), 7.20 (2H, quin), 4.50-4.00 (1H, obscured by water), 3.40 (1H, d), 3.20 (1H, d), 3.00-2.80 (2H, m), 2.10 (1H, m), 1.90 (1H, m), 1.75 (1H, m), 1.60 (1H, m).
184637-48-7 tert-Butyl 3-aminopiperidine-1-carboxylate 545809, apiperidines compound, is more and more widely used in various fields.
Reference£º
Patent; CELLTECH R & D LIMITED; WO2006/38001; (2006); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem