Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Toluene | HCID 1140 | — |
| Reactant | Potassium Phosphate, Tribasic | HCID 62657 | — |
| Reactant | HCID 86731462 | HCID 86731462 | — |
| Catalyst | Bis(cyclopenta-1,4-dien-1-yl(diphenyl)phosphane);dichloropalladium;iron(2+) | HCID 178418228 | — |
| Solvent | Water | HCID 962 | — |
| Product | HCID 86731463 | HCID 86731463 | 85% |
Reaction Steps
A mixture of ethyl 8-bromo-7-(4-(tert-butoxycarbonyl)piperazin-1-yl)isoquinoline-3-carboxylate (464 mg, 1 mmol), C3H4B(OH)2 (860 mg, 10 mmol), Pd(dppf)Cl2 (73 mg, 0.1 mmol) and K3PO4 (636 mg, 3 mmol) in toluene (20 ml) and H2O (2 ml) was stirred at 95° C. overnight. After extraction by EA, the residue was dried with anhydrous Na2SO4, concentrated in vacuo, and purified by silica gel chromatography to afford ethyl-7-(4-(tert-butoxycarbonyl)piperazin-1-yl)-8-cyclopropylisoquinoline-3-carboxylate as a yellow solid (350 mg, yield: 85%).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US09096549B2 |
|---|
| Source dataset | uspto-grants-2015_08 |
|---|
| ORD ID | ord-c02a0dd474164fbf8b899ef193d1fc8b |
|---|
| Source note | uspto-grants-2015_08 |
|---|
