Novel N-substituted piperazine derivatives containing sulfonyloxy aniline moiety have been prepared. The various 4-sulfonyloxy aniline (SA) derivatives (2a-h) have been prepared by the condensation reaction of N-Acetyl Sulfanilyl chloride (ASC) and sodium phenates followed by hydrolysis. The SA derivatives are then reacted with chloro acetyl chloride to give corresponding (N-Chloroacetyl) derivatives (3a-h). These derivatives are then reacted with N-phenyl piperazine to yield the corresponding piperazine derivatives (4a-h).