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[2-Fluoro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyridin-3-yl]-methyl-amine → 1-(1-Ethyl-3-methyl-1H-pyrazol-4-yl)-8-(6-fluoro-5-methylamino-pyridin-3-yl)-3-methyl-1,3-dihydro-imidazo[4,5-c]quinolin-2-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | [2-Fluoro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyridin-3-yl]-methyl-amine | HCID 59619630 | — |
| 反応物 | 8-bromo-1-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-3-methyl-1,3-dihydro-imidazo[4,5-c]quinolin-2-one | HCID 59619675 | — |
| 生成物 | 1-(1-Ethyl-3-methyl-1H-pyrazol-4-yl)-8-(6-fluoro-5-methylamino-pyridin-3-yl)-3-methyl-1,3-dihydro-imidazo[4,5-c]quinolin-2-one | HCID 59619621 | — |
反応手順
The title compound was synthesized in a similar manner as described for Example 1.1 using 8-bromo-1-(1-ethyl-3-methyl-1H-pyrazol-4-yl)-3-methyl-1,3-dihydro-imidazo[4,5-c]quinolin-2-one (Intermediate F, 0.078 mmol) and [2-fluoro-5-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-pyridin-3-yl]-methyl-amine (stage 150.1.1) to give the title compound as a yellow foam. (HPLC: tR 2.53 min (Method A); M+H=485 MS-ES; 1H-NMR (d6-DMSO, 400 MHz) 8.97 (s, 1H), 8.16 (s, 1H), 8.11-8.07 (m, 1H), 7.95-7.90 (m, 1H), 7.53-7.51 (m, 1H), 7.42-7.39 (m, 1H), 7.01-6.97 (m, 1H), 6.08 (q, br, 1H), 4.15 (q, 2H), 3.58 (s, 3H), 2.80 (d, 3H), 1.97 (s, 3H), 1.37 (t, 3H))
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08476294B2 |
| 出典データセット | uspto-grants-2013_07 |
| ORD ID | ord-2c17fa143c3a45c98d36b9ee5216329d |
| 出典メモ | uspto-grants-2013_07 |