1,2-Dichloroethane → HCID 68927242, compound

Participants

Reaction Steps

8-Piperidin-1-ylmethylchroman-4-ylamine dihydrochloride (Step E) (28 mg, 0.11 mmol), 3-(naphthalen-2-yl-sulfonylamino)-3-phenylpropionic acid (40 mg, 0.11 mmol), HOBt (17 mg, 0.12 mmol), and DIEA (21 mg, 0.16 mmol) were dissolved in CH2Cl2 (5 mL). EDC (25 mg, 0.13 mmol) was added and the reaction was kept at 22-25° C. overnight until completed. The reaction solution was washed with dilute (˜5%) NaHCO3—H2O and H2O, then dried over MgSO4, filtered and concentrated in vacuo to provide a residue which was purified by column chromatography (silica gel, 0.5% Et3N in EtOAc). The compound was converted to the HCl salt in Et2O to provide the title compound as a mixture of diastereomers, as a white solid (ca. 1:1 by 1H NMR). MS (ESI) 584 (M+H)+.

Provenance & Evidence