反应详情

256.4 mg (3.69 mmol) Hydroxylamine hydrochloride are added to a mixture of 1.0 g (3.69 mmol) (S)-N-{1-[4-(1-cyano-piperidin-4-yl)-phenyl]ethyl}-acetamide (XXVII.1) and 0.63 mL (3.69 mmol) DIPEA in 20 mL ethanol. The mixture is refluxed for 4 h, an additional amount of 50 mg hydroxylamine hydrochloride is added and refluxing is continued for 2 h. The solvent is removed in vacuo and water is added. The mixture is then purified by HPLC (RP C18 Xbridge, water (+0.1% ammonia)/MeOH) to yield the desired product.

1. temperatureThe mixture is refluxed for 4 h
2. temperaturerefluxing
3. customThe solvent is removed in vacuo and water
4. additionis added
5. customThe mixture is then purified by HPLC (RP C18 Xbridge, water (+0.1% ammonia)/MeOH)