Sodium Carbonate → (S)-2-(1-((6-Amino-5-(3-fluoro-5-hydroxyphenyl)pyrimidin-4-yl)amino)-3-(benzyloxy)propyl)-3-(3,5-difluorophenyl)-4-oxo-3,4-dihydropyrrolo[2,1-f][1,2,4]triazine-5-carbonitrile

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Reaction Steps

(S)-2-(1-((6-Amino-5-iodopyrimidin-4-yl)amino)-3-(benzyloxy)propyl)-3-(3,5-difluorophenyl)-4-oxo-3,4-dihydropyrrolo[2,1-f][1,2,4]triazine-5-carbonitrile (12 mg, 0.02 mmol) was treated with (3-fluoro-5-hydroxyphenyl)boronic acid (4.5 mg, 0.03 mmol), sodium carbonate (2 M, 55 μl, 0.11 mmol) and 2′-(dimethylamino)-2-biphenylyl-palladium(II) chloride dinorbornylphosphine complex (2 mg, 0.001 mmol) according to the method described in the Preparation 17. The residue was purified by reverse phase using SP1® Purification System to give 2 mg (18% yield) of the title compound as a white solid. Purity 97%.

Provenance & Evidence