Ethylamine → HCID 49773783, compound

Participants

Reaction Steps

4-{[6-(4-Fluoro-phenyl)-4-hydroxy-pyrido[3,2-d]pyrimidin-2-ylamino]-methyl}-benzenesulfonamide (100 mg, 0.23 mmol) and PyBOP (119 mg, 0.23 mmol) were taken up in DMF (2 mL) and DIEA (0.07 mL, 0.46 mmol) was added, followed by ethylamine (2.0M in THF) (0.115 mL, 0.23 mmol) This solution was stirred at room temperature overnight. The DMF was removed in vacuo and the residue diluted with ethyl acetate (2 mL) and washed with water and brine. The organic layer was dried over sodium sulfate and concentrated to afford an oily residue. The residue was purified by RP HPLC using a C18 column with a 0-60% gradient of 0.1% TFA-H2O/0.1% TFA-acetonitrile to afford 55 mg (52%) of Example 297. MS (m/z) 453.4 [M+H]+.

Provenance & Evidence