(R)-3,3-DifluorocyclopentanaMine hydrochloride synthesis

Yield: 82%

Reaction Conditions:

with hydrogenchloride in 1,4-dioxane at 0 - 20;

Steps:

1.4
Hydrochloric acid (4M in dioxane, 60 mL) was added to a solution of (R)-tert- butyl 3,3-difluorocyclopentylcarbamate (4.61 g, 20.8 mmol) in dioxane (40 mL) at 0 ⁰C. After complete addition, the reaction mixture was allowed to warm to room temperature and stirred for 2 hours. The solvent was removed in vacuo and the residue was triturated with diethylether to afford the title compound as an off-white solid (2.68 g, 82% yield). 1H NMR (CDCl₃, 400 MHz): δ 1.76-1.88 (IH, m), 2.10-2.40 (4H, m), 2.45-2.60 (IH, m), 3.68 (IH, quint), 8.33 (3H, s).

References:

Location in patent:Page/Page column 43