HuagongsheHuagongshe Chemistry Print Report · For research reference only
1-(4-(Trimethylstannyl)phenyl)piperidin-4-ol → (R)-tert-butyl 2-((7-(4-(4-hydroxypiperidin-1-yl)phenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 1-(4-(Trimethylstannyl)phenyl)piperidin-4-ol | HCID 71093682 | — |
| Reactant | (R)-tert-butyl 2-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate | HCID 86706988 | — |
| Catalyst | HCID 178418397 | HCID 178418397 | — |
| Solvent | Toluene | HCID 1140 | — |
| Product | (R)-tert-butyl 2-((7-(4-(4-hydroxypiperidin-1-yl)phenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate | HCID 86717400 | 27.6% |
Reaction Steps
1-(4-(trimethylstannyl)phenyl)piperidin-4-ol (398 mg, 1.17 mmol), (R)-tert-butyl 2-((7-chloropyrido[4,3-b]pyrazin-5-ylamino)methyl)morpholine-4-carboxylate (297 mg, 0.78 mmol), tetrakis(triphenylphosphine)palladium (180 mg, 0.15 mmol) were mixed in 5 mL toluene. The mixture was reacted at 100° C. overnight. Filtrated and concentrated, purified by flash chromatography (PE:EA=1:2) to give 112 mg reddish solid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09434726B2 |
| Source dataset | uspto-grants-2016_09 |
| ORD ID | ord-c0cad0a5575a4ad8be1364d8ccd5a2c8 |
| Source note | uspto-grants-2016_09 |