HuagongsheHuagongshe Chemistry Print Report · For research reference only
Cesium carbonate → 6-(4-(4-Acetylpiperazin-1-yl)phenylamino)-4-(thiophen-2-ylmethylamino)nicotinamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Cesium carbonate | HCID 10796 | — |
| Reactant | Binap, (A+-)- | HCID 634876 | — |
| Reactant | 1-[4-(4-Aminophenyl)piperazin-1-yl]ethan-1-one | HCID 736269 | — |
| Reactant | 6-Chloro-4-(thiophen-2-ylmethylamino)nicotinamide | HCID 58439831 | — |
| Catalyst | palladium(II) acetate | HCID 167845 | — |
| Solvent | 1,4-Dioxane | HCID 31275 | — |
| Product | 6-(4-(4-Acetylpiperazin-1-yl)phenylamino)-4-(thiophen-2-ylmethylamino)nicotinamide | HCID 67501584 | — |
Reaction Steps
A mixture of 6-chloro-4-(thiophen-2-ylmethylamino)nicotinamide (84 mg, 0.314 mmol), 1-(4-(4-aminophenyl)piperazin-1-yl)ethanone (82 mg, 0.374 mmol), Cs2CO3 (200 mg, 0.613 mmol), BINAP (35 mg, 0.056 mmol) and Pd(OAc)2 (25 mg, 0.111 mmol) in dioxane (2 mL) was degassed with Ar, then was stirred at 120 C for 3 h. The mixture was concentrated in vacuo. The residue was purified by HPLC to the titled compound (12 mg). MS 451.4 (M+H); UV 200.0, 244.3 nm; t 0.485 min.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09102625B2 |
| Source dataset | uspto-grants-2015_08 |
| ORD ID | ord-cbedb28fa18f430c937363c4b2863dc9 |
| Source note | uspto-grants-2015_08 |