反应详情

3-(1H-1,2,3-Triazol-4-yl)propanoic acid (step 2) (42 mg, 0.294 mmol) and 3,5-dichlorobenzyl 4-aminopiperidine-1-carboxylate hydrochloride (Example 17, step 2) (100 mg, 0.294 mmol) were dissolved in DMF (1 ml) and treated with DIPEA (257 μl, 1.472 mmol) followed by 50% T3P® solution in DMF (344 μl, 0.589 mmol). The reaction mixture was stirred at RT for 2 days and then concentrated under reduced pressure. The crude product was dissolved in DCM and washed with 10% citric acid. The organic portion was separated, dried over MgSO4 (anh), filtered and evaporated under reduced pressure. Purification by chromatography on silica eluting with 0-10% MeOH in EtOAc afforded the title compound;

1. concentrationconcentrated under reduced pressure
2. dissolutionThe crude product was dissolved in DCM
3. washwashed with 10% citric acid
4. customThe organic portion was separated
5. dry with materialdried over MgSO4 (anh)
6. filtrationfiltered
7. customevaporated under reduced pressure
8. customPurification by chromatography on silica eluting with 0-10% MeOH in EtOAc