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4-(Methylsulfonyl)phenylhydrazine hydrochloride → 7-fluoro-2-[1-(4-methylsulfonylphenyl)-3-difluoromethyl-1H-pyrazol-5-yl]benzothiazole
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-(Methylsulfonyl)phenylhydrazine hydrochloride | HCID 2735181 | — |
| 反応物 | 1-(7-Fluorobenzothiazol-2-yl)-4,4-difluorobutane-1,3-dione | HCID 23285386 | — |
| 生成物 | 7-fluoro-2-[1-(4-methylsulfonylphenyl)-3-difluoromethyl-1H-pyrazol-5-yl]benzothiazole | HCID 23285382 | 63% |
反応手順
The procedure of Example 9 was repeated using 1-(7-fluorobenzothiazol-2-yl)-4,4-difluorobutane-1,3-dione and 4-methylsulfonylphenylhydrazine hydrochloride as the starting materials to obtain 7-fluoro-2-[1-(4-methylsulfonylphenyl)-3-difluoromethyl-1H-pyrazol-5-yl]benzothiazole (yield, 63%). NMR(CDCl3) δ: 3.11 (3H, s), 6.81 (1H, t, J=54.8 Hz), 7.09 (1H, app t, J=8.6 Hz), 7.24 (1H, s), 7.48 (1H, dt, J=5.4 Hz, 8.0 Hz), 7.72-7.75 (3H, m), 8.03-8.07 (2H, m); mp 193-195° C. (methanol)
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06136831 |
| 出典データセット | uspto-grants-2000_10 |
| ORD ID | ord-28799ebfdfc345aaa09535da8ccc495e |
| 出典メモ | uspto-grants-2000_10 |