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1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide → N-Cyclopropyl-4-methoxy-2,6-dimethyl-N-({4-[(4-pyridin-3-ylpiperazin-1-yl)carbonyl]-1,3-oxazol-2-yl}methyl)benzenesulfonamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide | HCID 15908 | — |
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | 1-(Pyridin-3-yl)piperazine | HCID 437234 | — |
| 反応物 | 1-Hydroxybenzotriazole hydrate | HCID 2796029 | — |
| 反応物 | 2-({Cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,3-oxazole-4-carboxylic acid | HCID 58393098 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | N-Cyclopropyl-4-methoxy-2,6-dimethyl-N-({4-[(4-pyridin-3-ylpiperazin-1-yl)carbonyl]-1,3-oxazol-2-yl}methyl)benzenesulfonamide | HCID 58393276 | — |
反応手順
The title compound was prepared according to general procedure AH using 2-({cyclopropyl[(4-methoxy-2,6-dimethylphenyl)sulfonyl]amino}methyl)-1,3-oxazole-4-carboxylic acid (50 mg, 0.13 mmol), EDCI (50 mg, 0.26 mmol), HOBt monohydrate (40 mg, 0.26 mmol), DIPEA (90 μL, 0.52 mmol), 1-pyridin-3-ylpiperazine (21 mg, 0.13 mmol) and DMF (1 mL). The resulting crude compound was purified by FCC eluting with 99:1 DCM:7N NH3 in MeOH.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08623859B2 |
| 出典データセット | uspto-grants-2014_01 |
| ORD ID | ord-cd2762729c1b439cb88ea8116e06c5dd |
| 出典メモ | uspto-grants-2014_01 |