反应详情

A mixture of 1-{6-benzyloxy-1-[4-(2-pyrrolidin-1-yl-ethoxy)phenyl]-3,4-dihydro-1H-isoquinolin-2yl}-2,2,2-trifluoroethanone (1.088 g, 2.1 mmol) and anhydrous K2CO3 (2.861 g, 20.7 mmol) in MeOH (150 ml) was refluxed under N2 for 18 hr, then evaporated in vacuo to a yellow residue. This was dissolved in H2O (25 ml) and extracted with EtOAc (3×50 ml). The combined extracts were dried over MgSO4, and concentrated in vacuo to give 0.881 g of crude yellow product. Purification by flash chromatography, eluting first with EtOAc:MeOH (8:2), then with EtOAc:MeOH (1:1) gave 0.842 g (95% yield) of yellow oil.

1. temperaturewas refluxed under N2 for 18 hr
2. customevaporated in vacuo to a yellow residue
3. dissolutionThis was dissolved in H2O (25 ml)
4. extractionextracted with EtOAc (3×50 ml)
5. dry with materialThe combined extracts were dried over MgSO4
6. concentrationconcentrated in vacuo
7. customto give 0.881 g of crude yellow product
8. customPurification by flash chromatography
9. washeluting first with EtOAc:MeOH (8:2)