참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Sodium Carbonate | HCID 10340 | — |
| 반응물 | 1,2,4-Trifluoro-5-(methylsulfonyl)benzene | HCID 46739396 | — |
| 반응물 | (S)-1'-(5-ethylpyrimidin-2-yl)-3-(methylamino)-1,4'-bipiperidin-2-one | HCID 67470730 | — |
| 용매 | Dimethylformamide | HCID 6228 | — |
| 생성물 | HCID 86688112 | HCID 86688112 | 28% |
반응 단계
(S)-1′-(5-ethylpyrimidin-2-yl)-3-(methylamino)-1,4′-bipiperidin-2-one (0.040 g, 0.13 mmol), 1,2,4-trifluoro-5-(methylsulfonyl)benzene (Preparation C, 0.053 g, 0.25 mmol) and Na2CO3 (0.040 g, 0.38 mmol) were dissolved in DMF (1 mL) and heated at 130° C. overnight. The reaction was concentrated and the residue was purified using preparative TLC (100% EtOAc) to afford (S)-3-((2,5-difluoro-4-(methylsulfonyl)phenyl)(methyl)amino)-1′-(5-ethylpyrimidin-2-yl)-1,4′-bipiperidin-2-one (0.018 g, 0.035 mmol, 28% yield) as yellow solid. Mass spectrum (apci) m/z=508.3 (M+H).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US08754226B2 |
|---|
| 출처 데이터셋 | uspto-grants-2014_06 |
|---|
| ORD ID | ord-e88004b53ccb4100a1ec2b880703e257 |
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| 출처 메모 | uspto-grants-2014_06 |
|---|
