Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Methanol | HCID 887 | — |
| Reactant | Boron tribromide | HCID 25134 | — |
| Reactant | HCID 131736191 | HCID 131736191 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 118433836 | HCID 118433836 | 20% |
Reaction Steps
(S)—N-(6-(4-Amino-6-((1-(5-methyl-4-oxo-3-phenyl-3,4-dihydropyrrolo[2,1-f][1,2,4]triazin-2-yl)ethyl)amino)pyrimidin-5-yl)-1-((2-(trimethylsilyl)ethoxy)methyl)-1H-indol-4-yl)-4-methoxybenzenesulfonamide (56 mg, 0.07 mmol) was dissolved in dichloromethane (1 ml). A solution of boron tribromide (1M in dichloromethane, 707 μl, 0.71 mmol) was added dropwise and the reaction was stirred at room temperature overnight. Methanol was added and the solvents were removed. Then ammonia (7N in methanol) (1.5 ml) was added and the mixture was stirred at room temperature overnight. The solvent was removed and the residue was purified by reverse phase chromatography using SP1® Purification System to give 6 mg (20% yield) of the title compound as a white solid. Purity 97%.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US09388189B2 |
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| Source dataset | uspto-grants-2016_07 |
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| ORD ID | ord-3c3036cc8f9d46d093922ad9d18d389e |
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| Source note | uspto-grants-2016_07 |
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