Formic Acid → N-({4-Amino-7-[(4-formylpiperazin-1-yl)methyl]-5-(7-methoxy-5-methyl-1-benzothiophen-2-yl)-pyrrolo[2,1-f][1,2,4]triazin-6-yl}methyl)acetamide

Participants

Reaction Steps

Acetic acid anhydride (304 μl, 3.16 mmol) and formic acid (145 μl, 3.16 mmol) were stirred first 2 h at 50° C. and then overnight at rt. Subsequently, the mixture was diluted with dichloromethane (3.1 ml), and 663 μl of this solution were added to a solution of Example 63 (160 mg, 226 μmol) in pyridine (54 μl). The mixture was stirred at rt for 2 h, then diluted with methanol (1 ml), and stirring was continued at 40° C. for another 2 h. After evaporation, the residue was purified by preparative RP-HPLC (Reprosil C18, gradient 10-95% acetonitrile/0.1% aq. formic acid) affording 74 mg (61% of th.) of title compound.

Provenance & Evidence