1-(4-Fluorophenyl)-3-(piperidin-4-yl)urea hydrochloride synthesis

Yield:913634-46-5 96%

Reaction Conditions:

with hydrogenchloride in ethyl acetate;

Steps:

II.2

Compound II-b (4 g, 11.85 mmol) was dissolved in ethyl acetate (50 mL) and saturated with gaseous HCl, and the reaction mixture stirred until all of the starting material was consumed. The mixture was concentrated to give amine hydrochloride EPO salt as a white crystalline solid which was used in next step without further purification (3.1 g, 96%).[117] ¹H-NMR(D₂O): δ 7.59-7.68 (m, 2H), 7.01-7.13 (m, 2H), 3.98-4.10 (m, IH),3.35-3.44 (m, 2H), 2.94-3.07 (m, 2H), 2.05-2.14 (m, 2H), 1.62-1.75 (m, 2H).

References:

WO2006/115353,2006,A1 Location in patent:Page/Page column 12-13