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Diisopropylethylamine → N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-((1-tosyl-1H-indol-6-yl)methyl)pyrimidine-2,4-diamine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | (1-tosyl-1H-indol-6-yl)methanamine | HCID 71272360 | — |
| 反応物 | HCID 178478345 | HCID 178478345 | — |
| 溶媒 | 1-Butanol | HCID 263 | — |
| 生成物 | N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-((1-tosyl-1H-indol-6-yl)methyl)pyrimidine-2,4-diamine | HCID 86694718 | 96.4% |
反応手順
A microwave vial was charged with 53 (80 mg, 0.34 mmol), 36 (80 mg, 0.27 mmol), DIPEA (0.2 mL) and n-BuOH (2.0 mL), sealed and irradiated in a microwave reactor at 180° C. for 80 min. The reaction mixture was concentrated and purified with a CombiFlash® to afford 130 mg (95%) of N4-(5-cyclopropyl-1H-pyrazol-3-yl)-N2-((1-tosyl-1H-indol-6-yl)methyl)pyrimidine-2,4-diamine (38) as yellow solid; MS (ESI) m/z=500.1 [M+1]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08637537B2 |
| 出典データセット | uspto-grants-2014_01 |
| ORD ID | ord-4a9b58dc613a48b19e3819d5e555b259 |
| 出典メモ | uspto-grants-2014_01 |