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2-Vinylnaphthalene → 2-Ethyl-5-fluoro-9-methyl-13-[2-(naphthalen-2-yl)ethyl]-2,4,9,15-tetraazatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3(8),4,6,11,13-hexaen-10-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Vinylnaphthalene | HCID 13230 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | HCID 10807825 | HCID 10807825 | — |
| 触媒 | HCID 178418476 | HCID 178418476 | — |
| 生成物 | 2-Ethyl-5-fluoro-9-methyl-13-[2-(naphthalen-2-yl)ethyl]-2,4,9,15-tetraazatricyclo[9.4.0.0^{3,8}]pentadeca-1(15),3(8),4,6,11,13-hexaen-10-one | HCID 470740 | — |
反応手順
8-Bromo-2-fluoro-5,11-dihydro-11-ethyl-5-methyl-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-one (35 mg, 0.10 mmol) was coupled with 2-vinylnaphthalene in the presence of bis(triphenylphosphine)palladium(II) chloride and (i-Pr)2NEt as described in example 1h. The product was hydrogenated as described in example 3b. Purification by flash chromatography (elution with ethyl acetate-hexanes) and recrystallization (diethyl ether-hexanes) afforded 20 mg of the title compound as white crystals, m.p. 112°-114° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05705499 |
| 出典データセット | uspto-grants-1998_01 |
| ORD ID | ord-ab541c7440ab4735aed2d1ec4c86dad6 |
| 出典メモ | uspto-grants-1998_01 |