참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | 2-Bromo-3-chloropyridine | HCID 7016326 | — |
| 반응물 | (R)-3-Aminopiperidine-2-one | HCID 7200371 | — |
| 시약 | Sodium t-butoxide | HCID 23676156 | — |
| 촉매 | Binap, (A+-)- | HCID 634876 | — |
| 촉매 | Bis(dibenzylideneacetone)palladium | HCID 9811564 | — |
| 용매 | Toluene | HCID 1140 | — |
| 생성물 | HCID 178418225 | HCID 178418225 | 2% |
반응 단계
In a 5 ml MW vial, Pd2((dba)3 (7.23 mg, 7.90 µmol), 2,2'-bis(diphenylphosphanyl)-1,1'-binaphthalene (BINAP) (9.71 mg, 0.02 mmol), sodium 2-methylpropan-2-olate (174 mg, 1.81 mmol), (R)-3-aminopiperidin-2-one (119 mg, 1.04 mmol) and 2-bromo-3-chloropyridine (200 mg, 1.04 mmol) mixed in toluene (2 mL) to give a brown suspension. The mixture was degassed with N2 bubbling for 5 min, then the vial was capped and the reaction stirred at 115°C in an oil-bath over night. The reaction was cooled to rt, DCM and aq NaHCO3 were added, the mixture stirred, filtered through a phase separator and evaporated. LC-MS crude: Traces of product, mainly starting bromide left. Reaction discarded.
출처 및 근거
| 출처 데이터셋 | 750 AstraZeneca ELN dataset |
|---|
| ORD ID | ord-945adafe269741f9bc504b4e9b38a0a3 |
|---|
| 출처 메모 | 750 AstraZeneca ELN dataset |
|---|