4-Piperidinamine → HCID 10752643, compound

Participants

Reaction Steps

Using the procedure of Example 1, piperidin-4-ylamine Compound 21a1 was used in place of Compound 1n2 and carried forward to prepare 1-(4-nitro-benzyl)-piperidin-4-ylamine Compound 21a2. 5% Rh/C (350 mg) was added to a solution of 1-(4-nitrobenzyl)-piperidin-4-ylamine Compound 21a2 (647 mg, 2.75 mmol) in methanol (15 mL). The mixture was hydrogenated at 50 PSI for a period of 2 hrs, then filtered through Celite. The filtrate was evaporated in vacuo to give 1-(4-amino-benzyl)-piperidin-4-ylamine Compound 21a (640 mg) as a light yellow oil. 1H NMR (CDCl3) δ 7.09 (d, J=8.2 Hz, 2H); 6.64 (d, J=8.2 Hz, 2H); 3.62 (br s, 1H); 3.41 (s, 2H); 2.88-2.80 (m, 2H); 2.70-2.58 (m, 1H); 2.07-1.95 (m, 2H); 1.84-1.74 (m, 2H); 1.57 (br s, 2H); 1.47-1.32 (m, 2H); 1.31-1.18 (m, 2H).

Provenance & Evidence