1-ACETYL-4-BOCAMINO-PIPERIDINE

To a solution of ie -butyl piperidin-4-yl carbamate (5.0 g, 25 mmol) in DCM (80 mL) at 0 °C were added EtiN (3.8 g, 38 mmol) and AC2O (2.6 g, 25 mmol). The resulting mixture was stirred at 0 °C for 2 hours. The reaction was quenched with water (30 mL), separated and the organic layer was washed with saturated NaHCC>3 (30 mL), dried over a2S0Acetic anhydride (4.71 mL, 49.9 mmol) was added to a solution of terf-butyl piperidin-4- ylcarbamate (10.0 g, 49.9 mmol) and triethylamine (10.4 mL, 74.9 mmol) in anhydrous DCM (100 mL) at 0 °C. The reaction mixture was stirred at 0 C for 2 hours before water (-100 mL) and DCM (-50 mL) were added. The organic phase was separated, washed with a saturated aqueous NaHCC solution (-100 mL) and dried (MgS0To a solution of tert-butyl piperidin-4-ylcarbamate (5.0 g, 25.0 mmol) in DCM (80 mL) at 0 00 was added Et3N (3.8 g, 37.5 mmol) and Ac20 (2.6 g, 25.0 mmol). The mixture was stirred at 0 00 for 2 hours. The reaction was quenched by the addition of water (30 mL) and theorganic layer separated and washed with a saturated aqueous solution of NaHCO3 (30 mL), dried (Na2SO4), filtered and concentrated to give the title compound as a white solid (4.8 g, 80percent). LCMS: RT 1 .88 mm; m/z 265.1 [M+Na].To a stirred suspension of 4-boc aminopiperidine (CAS Number 73874-95-0, available from Combi Blocks) (5.00 g, 24.960 mmol) in dichloromethane (30 ml) was added triethylamine (10.40 ml, 74.88 mmol) and acetyl chloride (2.1 1 ml, 29.950 mmol) at 0°C and the resulting reaction mixture was stirred at room temperature for 1 h. The resulting reaction mixture was poured into water (100 ml) and extracted with dichloromethane (2 x 100 ml). The combined organic layer was dried over Na2S0

Molecular Weight:242.31
XLogP3:1
Hydrogen Bond Donor Count:1
Hydrogen Bond Acceptor Count:3
Rotatable Bond Count:3
Exact Mass:242.16304257
Monoisotopic Mass:242.16304257
Topological Polar Surface Area:58.6
Heavy Atom Count:17
Complexity:289
Covalently-Bonded Unit Count:1
Compound Is Canonicalized:Yes