참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Cesium carbonate | HCID 10796 | — |
| 반응물 | 4-Cyanophenylboronic acid | HCID 2734326 | — |
| 반응물 | HCID 178480720 | HCID 178480720 | — |
| 용매 | Dimethylformamide | HCID 6228 | — |
| 생성물 | HCID 178480723 | HCID 178480723 | 29.5% |
반응 단계
To a suspension of 6-bromo-4-{[4-(4-methyl-piperazin-1-yl)-phenylamino]-methylene}-4H-isoquinoline-1,3-dione (221 mg, 0.5 mmol) in N,N-dimethylformamide (5 mL) is added 4-cyanophenylboronic acid (88 mg, 0.6 mmol), followed by 300 □L of 2M aqueous cesium carbonate and tetrakis triphenylphosphine palladium (30 mg, 0.06 mmol). The reaction mixture is subjected to microwave heating at 180° C. for 300 seconds. The reaction mixture is then diluted with N,N-dimethylformamide and purified by C18 reverse phase HPLC. The pure fractions were combined and concentrated to yield 4-(4-{[4-(4-Methyl-piperazin-1-yl)-phenylamino]-methylene}-1,3-dioxo-1,2,3,4-tetrahydro-isoquinolin-6-yl)-benzonitrile (68.4 mg).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US07713994B2 |
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| 출처 데이터셋 | uspto-grants-2010_05 |
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| ORD ID | ord-3cfad6abb88d4c68b8c8ab7840ffd736 |
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| 출처 메모 | uspto-grants-2010_05 |
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