4-Methylmorpholine → HCID 50923462, compound

Participants

Reaction Steps

4a.2 146 mg of {4-[6-amino-5-(6-methoxy-1H-benzimidazol-2-yl)pyridin-3-yl]pyrazol-1-yl}acetic acid (0.120 mmol) are dissolved in 1.5 ml of DMF. 17.5 mg (0.120 mmol) of 3,4-difluorobenzylamine, 16.2 mg (0.120 mmol) of HOBt, 23 mg (0120 mmol) of EDC and 26.4 μl (0.240 mmol) of N-methylmorpholine are added. The reaction mixture is stirred at room temperature for 14 h, and water/ethyl acetate is subsequently added. The aqueous phase is extracted 2× with ethyl acetate. The combined organic phases are washed with water, dried using sodium sulfate, filtered and evaporated to dryness. The residue is purified by means of preparative RP-HPLC, giving 2-{4-[6-amino-5-(6-methoxy-1H-benzimidazol-2-yl)pyridin-3-yl]pyrazol-1-yl}-N-(3,4-difluorobenzyl)acetamide; HPLC-MS [M+H]+ 490.2;

Provenance & Evidence