Reaktion #71674

Reaktionsgleichung

2-methyl-3-pyridinecarboxylic acid

HATU

DIPEA

(2R)-2-methyl-1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine hydrochloride

→

title compound

Ausbeute 98.0%

(2R)-2-Methyl-4-[(2-methyl-3-pyridinyl)carbonyl]-1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine formic acid salt

Ausbeute 98.0%

Lösungsmittel

DCM

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   Einengenthe reaction mixture was then concentrated
2. 2
   Sonstigepurified by reverse phase MDAP
3. 3
   EinengenThe collected fractions were concentrated in vacuo

Vorschrift

To a solution of 2-methyl-3-pyridinecarboxylic acid (47.7 mg, 0.348 mmol) in DCM (2.000 ml) was added HATU (132 mg, 0.348 mmol) and DIPEA (0.152 ml, 0.870 mmol) and the mixture stirred for 15 minutes before addition of (2R)-2-methyl-1-{[4-(trifluoromethyl)phenyl]sulfonyl}piperazine hydrochloride (Description 6) (100 mg, 0.290 mmol) in DMF (2 ml). The resultant mixture was stirred for 16 h at room temperature then the reaction mixture was then concentrated and the residue taken up in DMSO and purified by reverse phase MDAP. The collected fractions were concentrated in vacuo giving the title compound (80.7 mg) as a white solid.

Quelle