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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 43392Generated: October 25, 2026

Water → 4-{5-[(4-{[4-(Trifluoromethyl)phenyl]sulfonyl}-1-piperazinyl)carbonyl]-2-pyridinyl}morpholine

https://huagongshe.com/reaction/43392

Reaction equation

Participants

RoleNameHCIDCharge
ReactantWaterHCID 962—
Reactant1-HydroxybenzotriazoleHCID 75771—
ReactantDiisopropylethylamineHCID 81531—
Reactant1-[4-(Trifluoromethyl)benzenesulfonyl]piperazineHCID 2554578—
ReactantMethanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 2733084—
Reactant6-Morpholinonicotinic AcidHCID 2776460—
SolventDimethylformamideHCID 6228—
Product4-{5-[(4-{[4-(Trifluoromethyl)phenyl]sulfonyl}-1-piperazinyl)carbonyl]-2-pyridinyl}morpholineHCID 2611210278.2%

Reaction Steps

To a solution of 1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine (Description 1) (80 mg, 0.272 mmol) in DMF (5 ml) were added 6-(4-morpholinyl)-3-pyridinecarboxylic acid (56.6 mg, 0.272 mmol), HOBT.H2O (41.6 mg, 0.272 mmol), HBTU (103 mg, 0.272 mmol) and DIPEA (0.142 ml, 0.816 mmol) and the reaction mixture was stirred at room temperature for 2 h. The DMF was evaporated in vacuo then 5 ml of DCM were added and washed with saturated aqueous 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 (103 mg).

Provenance & Evidence

DOI10.6084/m9.figshare.5104873.v1
Patent numberUS08536183B2
Source datasetuspto-grants-2013_09
ORD IDord-c38249caf2674a54ad692beb27cfd819
Source noteuspto-grants-2013_09