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1-[[4-(TRIFLUOROMETHOXY)PHENYL]SULFONYL]PIPERAZINE synthesis

3synthesis methods
1-Piperazinecarboxylic acid, 4-[[4-(trifluoromethoxy)phenyl]sulfonyl]-, 1,1-dimethylethyl ester

847039-26-3
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1-[[4-(TRIFLUOROMETHOXY)PHENYL]SULFONYL]PIPERAZINE

756859-05-9
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Yield:756859-05-9 87%

Reaction Conditions:

with trifluoroacetic acid in dichloromethane at 0; for 1 h;

Steps:

40.B

To a cold (0 C) solution of 4- (4-TRIFLUOROMETHOXY-BENZENESULFONYL)-PIPERAZINE- 1-carboxylic acid tert-butyl ester (1.15 g, 2.8 MMOL) in DCM (3 ml) was added TFA (2 ml). The resulting solution was stirred for 1 hr. Solvent was then removed under reduced pressure. The crude solid was taken-up in AcOEt (15 ML) and washed with NAHCO3 SAT (2 X 5 ML), water (5 ML) and finally with brine (5 ml). The organic layer was dried over MGS04 and the solvent was removed under vacuo to yield the desired 1- (4-TRIFLUOROMETHOXY-BENZENESULFONYL)- piperazine as a white solid (753 mg, 87% yield).

References:

WO2005/19194,2005,A1 Location in patent:Page/Page column 51-52