反应详情

A mixture of 3-tert-butyl aniline (54 mg, 0.36 mmol), 1-(4-carboxy-phenyl)-piperidine-4-carboxylic acid ethyl ester (100 mg, 0.36 mmol) and EDCI (200 mg, 1.08 mmol) in CH2Cl2 was stirred at room temperature overnight. Next morning the reaction mixture was partitioned between EtOAc and water. The organic layer was separated dried over Na2SO4, filtered and concentrated. The residue was purified on a silica gel column with 20-50% Et2O in hexanes gradient to afford the product (31 mg; Yield: 21%). HRMS m/z calcd for C25H32N2O3 [M+H]+: 409.2486. Found: 409.2484.

1. customNext morning the reaction mixture was partitioned between EtOAc and water
2. customThe organic layer was separated
3. dry with materialdried over Na2SO4
4. filtrationfiltered
5. concentrationconcentrated
6. customThe residue was purified on a silica gel column with 20-50% Et2O in hexanes gradient
7. customto afford the product (31 mg; Yield: 21%)