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Pipemidic Acid → 2-(4-{[(4-Morpholinosulfonylphenyl)amino]carbonothioyl}-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic Acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Pipemidic Acid | HCID 4831 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 4-[(4-Isothiocyanatophenyl)sulfonyl]morpholine | HCID 3725513 | — |
| 生成物 | 2-(4-{[(4-Morpholinosulfonylphenyl)amino]carbonothioyl}-1-piperazinyl)-8-ethyl-5-oxo-5,8-dihydropyrido[2,3-d]pyrimidine-6-carboxylic Acid | HCID 86664291 | 87.3% |
反応手順
Pipemidic acid (14.2 mg, 0.0468 mmol), 4-(morpholinosulfonyl)phenyl isothiocyanate (14 mg, 0.0468 mmol) and triethylamine (13 μL, 0.0935 mmol) were used. Purification on silica yielded 6 (24 mg, 85%). 1H NMR (300 MHz, CDCl3) δ 9.28 (s, 1H), 8.65 (s, 1H), 8.09 (s, 1H), 7.64 (d, J=8.71 Hz, 2H), 7.51 (d, J=8.61 Hz, 2H), 4.43-4.01 (m, 10H), 3.80-3.70 (m, 4H), 3.04-2.98 (m, 4H), 1.49 (t, J=7.17 Hz, 3H) ppm.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08497371B2 |
| 出典データセット | uspto-grants-2013_07 |
| ORD ID | ord-a5633ed7e8b94343905b7ba0eea45b54 |
| 出典メモ | uspto-grants-2013_07 |