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2-Amino-4,6-dimethoxypyrimidine → 4-(Cyclopropylcarbonyl)-N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1-methyl-1H-pyrazole-5-sulfonamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Amino-4,6-dimethoxypyrimidine | HCID 118946 | — |
| 反応物 | 4-Cyclopropylcarbonyl-1-methyl-5-pyrazolesulfonamide | HCID 14230998 | — |
| 反応物 | Phenylcarbamate | HCID 21896570 | — |
| 反応物 | HCID 22171225 | HCID 22171225 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 4-(Cyclopropylcarbonyl)-N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1-methyl-1H-pyrazole-5-sulfonamide | HCID 14230999 | — |
反応手順
To a stirring mixture of the sulfonamide from Example 2 (175 mg, 0.76 mmol) and the phenylcarbamate of 4,6-dimethoxy-2-aminopyrimidine (210 mg, 0.76 mmol) in 3ml of acetonitrile was added diazobicycloundecane (116 mg, 0.76 mmol). The solution was stirred for approximately 10 minutes. Acidification of the reaction mixture and filtration of the resulting solids afforded 300 mg of the desired compound m.p. 189°-192° C. NMR (200 MHz, CDCl3) 1.0 (m, 2H), 1.1 (m, 2H), 2.4 (m, 1H), 4.0 (s, 6H), 4.35 (s, 1H), 5.80 (s, 1H), 7.4 (br. s, 1H), 8.05 (s, 1H), 12.9 (s, 1H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04747870 |
| 出典データセット | uspto-grants-1988_05 |
| ORD ID | ord-f761c60319374e4c9f87c57163d94478 |
| 出典メモ | uspto-grants-1988_05 |