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N-acetylanthranilic acid → 5-Methyl-6-(2-methyl-4-oxo-4H-quinazolin-3-yl)-4-(4-phenoxy-phenylamino)-pyrrolo[1,2-b]pyridazine-3-carbonitrile
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | N-acetylanthranilic acid | HCID 6971 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | PyBOP | HCID 2724699 | — |
| 反応物 | 6-Amino-5-methyl-4-(4-phenoxy-phenylamino)-pyrrolo[1,2-b]pyridazine-3-carbonitrile hydrochloride | HCID 22179487 | — |
| 溶媒 | 1,2-Dichloroethane | HCID 11 | — |
| 生成物 | 5-Methyl-6-(2-methyl-4-oxo-4H-quinazolin-3-yl)-4-(4-phenoxy-phenylamino)-pyrrolo[1,2-b]pyridazine-3-carbonitrile | HCID 22179517 | — |
反応手順
6-Amino-5-methyl-4-(4-phenoxy-phenylamino)-pyrrolo[1,2-b]pyridazine-3-carbonitrile hydrochloride (10.4 mg, 0.027 mmol), 2-acetylamino benzoic acid (7 mg, 0.04 mmol), PyBOP (21 mg, 0.04 mmol) and DIEA (8.6 mg, 0.067 mmol) in 1.2-dichloroethane (0.5 ml) were stirred at RT for 16 hrs. The reaction mixture was concentrated and purified by silica gel flash chromatography to isolate 375 as a yellow film (5.8 mg, 42%). [M+H]+=498.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07030112B2 |
| 出典データセット | uspto-grants-2006_04 |
| ORD ID | ord-ec285a38b7bb45b8a73d88a8383359ef |
| 出典メモ | uspto-grants-2006_04 |