Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sodium Carbonate | HCID 10340 | — |
| Reactant | Boronic Acid | HCID 61668 | — |
| Reactant | 1,4-Dioxane--water (1/1) | HCID 21886435 | — |
| Reactant | HCID 70872611 | HCID 70872611 | — |
| Catalyst | HCID 178418397 | HCID 178418397 | — |
| Solvent | Water | HCID 962 | — |
| Product | HCID 70872705 | HCID 70872705 | 68.66% |
Reaction Steps
To a stirred solution of tert-butyl 4-((5-bromo-3-(((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)carbamoyl)-2-methyl-phenyl)(ethyl)amino)piperidine-1-carboxylate (2 g, 3.47 mmol) and 4-(morpholinomethyl)-phenyl)boronic acid (1.58 g, 5.21 mmol) in dioxane/water mixture, Na2CO3 (1.32 g, 12.45 mmol) was added and solution purged with argon for 15 min. Then Pd(PPh3)4 (0.4 g, 0.35 mmol) was added and argon was purged again for 10 min. The reaction mixture was heated at 90° C. for 3.5 h. On completion, reaction mixture was diluted with water and extracted with 10% MeOH/DCM. Combined organic layers were dried over Na2SO4 and solvent removed under reduced pressure to afford crude material which was purified by column chromatography over silica gel to afford desired compound (1.6 g, 68.66%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US08765732B2 |
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| Source dataset | uspto-grants-2014_07 |
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| ORD ID | ord-92d1055571484711aff4de8e960a5bae |
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| Source note | uspto-grants-2014_07 |
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