반응 #1139599

반응 방정식

(S)-2-(1-((5-Bromo-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)ethyl)-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4(3H)-one

(3-(methylsulfonamido)phenyl)boronic acid

sodium carbonate

→

title compound

수율 76.9%

(S)—N-(3-(4-((1-(5-Methyl-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl)amino)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)phenyl)methanesulfonamide

수율 76.9%

반응 조건

후처리

1. 1
   기타described in Preparation 62
2. 2
   기타The residue was purified
3. 3
   기타SP1® Purification System (0% to 25%, dichloromethane-ethyl acetate)

실험 절차

(S)-2-(1-((5-Bromo-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-4-yl)amino)ethyl)-5-methyl-3-phenylpyrrolo[2,1-f][1,2,4]triazin-4(3H)-one (90 mg, 0.15 mmol) was treated with (3-(methylsulfonamido)phenyl)boronic acid (216 mg, 0.73 mmol), sodium carbonate (77 mg, 0.73 mmols) and bis(triphenylphosphine)palladium(II) dichloride (22 mg, 0.03 mmol) according to the method described in Preparation 62. The residue was purified using SP1® Purification System (0% to 25%, dichloromethane-ethyl acetate) to give 79 mg (73% yield) of the title compound. Purity 95%.

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