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HuagongsheHuagongshe Chemistry Print Report · For research reference only
HRID 2066120Generated: October 26, 2026

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

https://huagongshe.com/reaction/2066120

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 numberUS08288388B2
Source datasetuspto-grants-2012_10
ORD IDord-96a7ee4c63ff4c868f7d9a88b6cda8c4
Source noteuspto-grants-2012_10