5-Fluoro-3-phenyl-1-(piperidin-1-ylmethyl)-1H-indazole synthesis

Yield:-

Reaction Conditions:

with sodium hydroxide;paraformaldehyde in ethanol;benzene;

Steps:

36 EXAMPLE 36

EXAMPLE 36 3-Phenyl-5-fluoroindazole (2.12 g), paraformaldehyde (0.33 g), piperidine (1 g) and 1N aqueous sodium hydroxide solution (1 ml) were added to ethanol (30 ml) followed by heating under reflux for 3 hours. The reaction mixture was concentrated under reduced pressure and the residue was dissolved in benzene, washed with water, dried over sodium sulfate and concentrated under reduced pressure to obtain 1.9 g of 1-piperidinomethyl-3-phenyl-5-fluoroindazole having a melting point between 82°-84° C after recrystallization from methanol. Analysis: Calcd. for C₁₉ H₂₀ N₃ F: C, 73.76; H, 6.52; N, 13.58 (%) Found: C, 73.94; H, 6.46; N, 13.83 (%)

References:

US3994890,1976,A