反应详情

A solution of trans-4-({2-[2-(Carboxy-methyl-amino)-phenyl]-acetylamino}-methyl)-cyclohexanecarboxylic acid (0.14 mmol, 0.05 g) in SOCl2 (0.8 mL) was heated under reflux for 1.5 hours. The solvent was removed under reduced pressure and the residue was put under vacuum overnight. Then crude product was diluted with 5 ml of dry DCM. 1 ml of this stock solution was transferred in a glass vial. 39 μL (0.27 mmol) of 1-Pyridin-2-yl-piperazine were added and the reaction mixture was left stirring at room temperature under argon over night. The solvent was removed under vacuum and the crude purified by preparative HPLC (Method d) to give 26 mg of the titled compound (yield 39%).

1. temperatureunder reflux for 1.5 hours
2. customThe solvent was removed under reduced pressure
3. customwas put under vacuum overnight
4. additionThen crude product was diluted with 5 ml of dry DCM
5. waitthe reaction mixture was left
6. customThe solvent was removed under vacuum
7. customthe crude purified by preparative HPLC (Method d)