참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | o-Bromocumene | HCID 23475 | — |
| 반응물 | Dimethoxyethane ethanol | HCID 20074477 | — |
| 반응물 | 4-(3'-Benzylphenyl)-3-(S)-isopropyl-piperazine | HCID 20760004 | — |
| 반응물 | Sodium t-butoxide | HCID 23676156 | — |
| 촉매 | 2'-(diphenylphosphanyl)-N,N-dimethyl-[1,1'-biphenyl]-2-amine | HCID 2734939 | — |
| 용매 | Toluene | HCID 1140 | — |
| 용매 | Diethyl Ether | HCID 3283 | — |
| 생성물 | 1-(3-Benzyl-phenyl)-2-(S)-isopropyl-4-(2-isopropyl-phenyl)-piperazine | HCID 69129555 | 62.2% |
반응 단계
110.7 mg (0.38 mmol) 4-(3′-Benzylphenyl)-3-(S)-isopropyl-piperazine (88a), 123.5 mg (0.62 mmol, 1.65 eq.) 1-Bromo-2-isopropyl-benzene 11.7 mg (12.7 μmol, 0.034 eq.) Pd2(dba)3, 7.4 mg (19.3 μmol, 0.05 eq.) 2-Diphenylphosphino-2′-dimethylamino-biphenyl and 87.3 mg (0.91 mmol, 2.42 eq.) NaOt-Bu were dissolved in 5 ml dry toluene. The resulting mixture was heated under N2 at 80° C. for 15.5 h. After cooling to room temperature the mixture was diluted with ether and washed with brine. The comb. org. fractions were dried over Na2SO4 and evaporated. Column chromatography (hexanes/EtOAc (9+1)) yielded 96.5 mg (0.23 mmol, 62.20%) 1-(3-Benzyl-phenyl)-2-(S)-isopropyl-4-(2-isopropyl-phenyl)-piperazine (89) as a clear oil.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US07312246B2 |
|---|
| 출처 데이터셋 | uspto-grants-2007_12 |
|---|
| ORD ID | ord-22028e2f0fd24a9189311b03f7571aaf |
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| 출처 메모 | uspto-grants-2007_12 |
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