HuagongsheHuagongshe Chemistry Print Report · For research reference only
Tributylphosphine → 4-[(5-chlorothiophen-2-yl)methoxy]-1-(2-cyclopropyl-3-methyl-2H-indazol-5-yl)pyridin-2(1H)-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Tributylphosphine | HCID 13831 | — |
| Reactant | 1,1'-(Azodicarbonyl)dipiperidine | HCID 73042 | — |
| Reactant | (5-Chlorothiophen-2-yl)methanol | HCID 12554178 | — |
| Reactant | 1-(2-cyclopropyl-3-methyl-2H-indazol-5-yl)-4-hydroxypyridin-2(1H)-one | HCID 117798683 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | 4-[(5-chlorothiophen-2-yl)methoxy]-1-(2-cyclopropyl-3-methyl-2H-indazol-5-yl)pyridin-2(1H)-one | HCID 117798623 | 20.5% |
Reaction Steps
To a solution of 1-(2-cyclopropyl-3-methyl-2H-indazol-5-yl)-4-hydroxypyridin-2(1H)-one (70 mg) in tetrahydrofuran (5 ml) were added (5-chlorothiophen-2-yl)methanol (74 mg), 1,1′-(azodicarbonyl)dipiperidine (188 mg) and tributylphosphine (151 mg) at room temperature, and the mixture was stirred at the same temperature for 3 hr. The reaction mixture was purified by silica gel column chromatography (methanol/ethyl acetate) to give the title compound (21 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09199963B2 |
| Source dataset | uspto-grants-2015_12 |
| ORD ID | ord-f5eb3606e81049b28d85202723ee367b |
| Source note | uspto-grants-2015_12 |