Yield:546116-24-9 70%

Reaction Conditions:

Stage #1: 1-(o-fluorophenyl)piperazinewith triethylamine in diethyl ether at 20; for 0.166667 h;
Stage #2: chloroacetyl chloride in diethyl ether at 20; for 2 h;

Steps:

1-(2-Chloro-1-oxoethyl)-4-arylsubstituted-piperazine(4a, b)

General procedure: Ten millimoles of 1-(2-fluorophenyl)piperazine(for 4a) or 1-(2-pyrimidin)piperazine (for 4b) was dissolved in 40 mL of diethyl ether with addition of 1.4 mL of triethylamine and stirred slowly at room temperature for 10 min. Then, 1.6 mL (20mmol) of chloroacetyl chloride in 20 mL of diethylether were slowly instilled, and stirring was continuedfor another 2 h. After this time, diethyl ether was evaporated in vacuum and 10 mL of water and 60 mL of chloroform were added. The organic phasewas separated, dried with MgSO4 and evaporated invacuum to give 4a or 4b.

References:

Szczesniak-siga, Berenika;Maniewska, Jadwiga;Pola, Andrzej;rodapomianek, Kamila;Malinka, Wieslaw;Michalak, Krystyna [Acta poloniae pharmaceutica,2014,vol. 71,# 6,p. 1045 - 1050]