反应详情

7-(5-{3-Chloro-4-[(1-methylethyl)oxy]phenyl}-1,2,4-oxadiazol-3-yl)-2,3,4,5-tetrahydro-1H-3-benzazepine hydrochloride (Example 17) (65 mg, 0.155 mmol), DIPEA (0.104 ml, 0.593 mmol) and ethyl 4-bromobutanoate (0.048 ml, 0.339 mmol) were stirred at 60° C. in DMF (10 ml) for 24 hours. The reaction mixture was partitioned between EtOAc (˜30 ml) and water (˜30 ml) and the aqueous layer extracted once more with EtOAc (˜40 ml). The combined organics were concentrated in vacuo to yield the crude title compound (100 mg, 0.171 mmol) as an orange solid. MS (ES): C27H3235ClN3O4 requires 497; found 498 [M+H]+.

1. customThe reaction mixture was partitioned between EtOAc (˜30 ml) and water (˜30 ml)
2. extractionthe aqueous layer extracted once more with EtOAc (˜40 ml)
3. concentrationThe combined organics were concentrated in vacuo