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HuagongsheHuagongshe Chemie-Druckbericht · Nur für Forschungszwecke
HRID 41314Erstellt: 23. Oktober 2026

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

https://huagongshe.com/de/reaction/41314

Reaktionsgleichung

Beteiligte Stoffe

RolleNameHCIDEinwaage
EduktWaterHCID 962—
Edukt1-HydroxybenzotriazoleHCID 75771—
EduktDiisopropylethylamineHCID 81531—
EduktMethanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 2733084—
Edukt2-Methylpyridine-4-carboxylic acidHCID 2762821—
Edukt(S)-3-Methyl-1-((4-(trifluoromethyl)phenyl)sulfonyl)piperazineHCID 59152086—
LösungsmittelDimethylformamideHCID 6228—
Produkt(2S)-2-methyl-1-[(2-methyl-4-pyridinyl)carbonyl]-4-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine formic acid saltHCID 44612081120,7%

Reaktionsschritte

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-methyl-4-pyridinecarboxylic acid (35.6 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 DCM (5 ml) was added and washed with saturated aq. 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 in vacuo giving the title compound (74 mg).

Herkunft & Nachweise

DOI10.6084/m9.figshare.5104873.v1
PatentnummerUS08530478B2
Quelldatensatzuspto-grants-2013_09
ORD IDord-43d2502aae1d4b49bf668f12fc6946c8
Quellennotizuspto-grants-2013_09