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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 41308Generated: October 26, 2026

Water → (2S)-2-methyl-1-(2-pyridinylcarbonyl)-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine formic acid salt

https://huagongshe.com/reaction/41308

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
ReactantPicolinic acidHCID 1018—
Reactant1-HydroxybenzotriazoleHCID 75771—
ReactantDiisopropylethylamineHCID 81531—
ReactantMethanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 2733084—
Reactant(S)-3-Methyl-1-((4-(trifluoromethyl)phenyl)sulfonyl)piperazineHCID 59152086—
SolventDimethylformamideHCID 6228—
Product(2S)-2-methyl-1-(2-pyridinylcarbonyl)-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine formic acid saltHCID 44611963156.3%

Reaction Steps

To a solution of (3S)-3-methyl-1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (Description 2) (80 mg, 0.259 mmol) in DMF (5 ml) was added 2-pyridinecarboxylic acid (31.9 mg, 0.259 mmol), HOBT.H2O (39.7 mg, 0.259 mmol), HBTU (98 mg, 0.259 mmol) and DIPEA (0.136 ml, 0.778 mmol) and the reaction mixture was stirred at room temperature overnight. DMF was evaporated in vacuo then 5 ml of DCM were added and washed with saturated NaHCO3 solution (5 ml), dried on a phase separation cartridge and evaporated in vacuo. The crude material was dissolved in MeCN/DMSO 1:1 and purified by MDAP. The desired fractions were collected and concentrated under vacuo giving the title compound (93 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08530478B2
Source datasetuspto-grants-2013_09
ORD IDord-3fdf3a4d29164d49ac70013b48cdf0ee
Source noteuspto-grants-2013_09