Dimethylformamide → HCID 63750403, compound

Participants

Reaction Steps

To a stirred solution of R-5 (100 mg, 0.62 mmol) in anhydrous DMF (3 mL) is added HATU (472 mg, 1.24 mmol) and DIPEA (322 mL, 1.86 mmol) and the reaction is stirred at room temperature for 1 h. 2-(Methylamino)ethanol (100 mL, 1.24 mmol) is added and the mixture is stirred at room temperature for 16 h. The reaction is diluted with DCM and saturated aqueous NaHCO3, the layers separated, and the aqueous solution extracted with further DCM. Combined organics are washed with saturated aqueous NaHCO3, and brine. NaCl is then added to the combined aqueous phases and then the aqueous solution extracted with EtOAc. Combined organics are washed with brine, dried over anhydrous Na2SO4 and concentrated in vacuo to give the title intermediate I-6 (379.4 mg) m/z 219.0 [M+H].

Provenance & Evidence