反应详情

To a solution of (Trans)-2-(4-(3-bromobenzyloxy)phenyl)cyclopropanamine (2 g, 6.2 mmol) and 2-cyclohexylacetaldehyde (790 mg, 6.2 mmol) in DCE (20 mL) sodium triacetoxy borohydrate (2.3 g, 2 equiv) was added slowly at 0° C. and stirred for 20 h. After completion, the reaction mixture was evaporated. The residue was dissolved in Methanol (15 mL) and NaBH4 (627 mg, 3 equiv) was added slowly at 0° C. to the reaction mixture and stirred for 3 h. After completion, the reaction mixture was poured into ice water (50 mL) and extracted with EtOAc (2×50 mL). The combined organic layers were washed with brine (50 mL) and dried over anhydrous Na2SO4, filtered and evaporated. The crude residue was purified by flash column chromatography by using EtOAc: Pet ether to get (Trans)-2-(4-(3-bromobenzyloxy) phenyl)-N-(2-cyclohexylethyl)cyclopropane amine (500 mg, 21%) as a pale yellow liquid.

1. customAfter completion, the reaction mixture was evaporated
2. dissolutionThe residue was dissolved in Methanol (15 mL)
3. stirringstirred for 3 h
4. extractionextracted with EtOAc (2×50 mL)
5. washThe combined organic layers were washed with brine (50 mL)
6. dry with materialdried over anhydrous Na2SO4
7. filtrationfiltered
8. customevaporated
9. customThe crude residue was purified by flash column chromatography