(4-fluorophenyl)[4-(pyridin-2-yl)piperazin-1-yl]methanone synthesis

Yield:332168-99-7 77%

Reaction Conditions:

with polymer-supported N-methylmorpholine in dichloromethane; for 16 h;

Steps:

(1-Acetyl-4-(5-nitropyridin-2-yl)piperazine) 5a

(General acetylation/sulphonylation procedure). Compound 3b (208 mg, 1 mmol), acetyl chloride (79 μl, 1.1 mmol) and PS-NMM (100 mg) in CH₂Cl₂ (5 mL) were stirred for 16 h. After adding PS-Trisamine (150 mg) to the reaction mixture was left to stir for a further 2 h, filtered and concentrated in vacuum to afford a yellow solid: 250 mg (90%) yield.

References:

Spencer, John;Patel, Hiren;Callear, Samantha K.;Coles, Simon J.;Deadman, John J. [Tetrahedron Letters,2011,vol. 52,# 45,p. 5905 - 5909] Location in patent:supporting information; experimental part