Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Dichloromethane | HCID 6344 | — |
| Reactant | Potassium Carbonate | HCID 11430 | — |
| Reactant | 1-(2-Bromo-5H-pyrrolo[2,3-b]pyrazin-7-yl)-2,2-dimethylpropan-1-one | HCID 57829218 | — |
| Reactant | HCID 59541021 | HCID 59541021 | — |
| Catalyst | Bis(cyclopenta-1,4-dien-1-yl(diphenyl)phosphane);dichloropalladium;iron(2+) | HCID 178418228 | — |
| Solvent | Water | HCID 962 | — |
| Solvent | 1,4-Dioxane | HCID 31275 | — |
| Product | HCID 67345197 | HCID 67345197 | 24% |
Reaction Steps
A mixture of 1-(2-bromo-5H-pyrrolo[2,3-b]pyrazin-7-yl)-2,2-dimethyl-propan-1-one (55 mg, 0.2 mmol), 1-[3-methoxy-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-phenyl]-pyrrolidine (67 mg, 0.22 mmol), potassium carbonate (70 mg, 0.51 mmol), Pd(dppf)Cl2.CH2Cl2 (12 mg, 0.015 mmol), 1.5 mL dioxane and 0.3 mL water was stirred at 160° C. in a microwave for 30 min. The resulting mixture was partitioned between ethyl acetate and water. The combined organic layers were dried over Na2SO4 and concentrated to give a dark brown residue. The crude product was purified by preparative thin layer chromatography using 140:9.5:0.5 CH2Cl2:MeOH:conc NH4OH as eluant. The resultant brown solid was washed with ethyl ether to provide 18 mg (24%) of 1-[2-(3-methoxy-3-pyrrolidin-1-yl-phenyl)-5H-pyrrolo[2,3-b]pyrazin-7-yl]-2,2-dimethyl-propan-1-one as a yellow solid. MP 245-256° C., M+H 379.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08008298B2 |
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| Source dataset | uspto-grants-2011_08 |
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| ORD ID | ord-0b352ef859084e329719749d08907a66 |
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| Source note | uspto-grants-2011_08 |
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