1,2-Dichloroethane → tert-Butyl (2-{2-[(4-{[(benzylamino)carbonyl]amino}benzyl)-amino]-2-oxoethyl}-1-oxo-2,3,4,5-tetrahydro-1H-2-benzazepin-5-yl)acetate

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Reaction Steps

130 mg (0.39 mmol) of the acid 3 are dissolved in 30 ml of CH2Cl2 and 0.07 ml of HUnig base and 77 mg of EDC (0.4 mmol) are added at 0° C. After 1 h, 100 mg of amine 5 dissolved in 10 ml of DMF are added dropwise and the mixture is stirred for a further 1 h. It is stirred at room temp. for 16 h, the solution is then concentrated, the residue is taken up in CH2Cl2/water and the mixture is washed with 1% citric acid, 5% NaHCO3 solution and water. The organic phase is dried and concentrated (92 mg).

Provenance & Evidence