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Triethylamine → 3-{4-[3-(5-tertbutyl-2-p-tolyl-2H-pyrazol-3-yl)ureido]phenyl}-1H-indole-2-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Triphosgene | HCID 94429 | — |
| 反応物 | 3-tert-butyl-1-(4-methylphenyl)-1H-pyrazol-5-amine | HCID 2974132 | — |
| 反応物 | 3-(4-Aminophenyl)-1H-indole-2-carboxamide | HCID 57762833 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | 3-{4-[3-(5-tertbutyl-2-p-tolyl-2H-pyrazol-3-yl)ureido]phenyl}-1H-indole-2-carboxamide | HCID 11555233 | 204.3% |
反応手順
43 mg of triphosgene followed by 110 μl of triethylamine at 0° C. are added to a solution of 100 mg of 3-(4-aminophenyl)-1H-indole-2-carboxamide (example 1) in 18 ml of tetrahydrofuran. The mixture is stirred for one hour at ambient temperature and then 110 mg of 5-tert-butyl-2-p-tolyl-2H-pyrazol-3-ylamine are added. The mixture is stirred for one hour and concentrated under reduced pressure, and the residue is triturated with 2 ml of ethyl acetate, to give a white solid. After filtration and drying, 150 mg of 3-{4-[3-(5-tertbutyl-2-p-tolyl-2H-pyrazol-3-yl)ureido]phenyl}-1H-indole-2-carboxamide are obtained, the characteristics of which are as follows:
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07566736B2 |
| 出典データセット | uspto-grants-2009_07 |
| ORD ID | ord-1accc1a177e347c69da15df7b1b259c9 |
| 出典メモ | uspto-grants-2009_07 |