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4-(Trifluoromethyl)phenyl isocyanate → 1-[3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-3-(4-trifluoromethyl-phenyl)-urea
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-(Trifluoromethyl)phenyl isocyanate | HCID 73768 | — |
| 反応物 | 3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenylamine | HCID 46929183 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | 1-[3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-3-(4-trifluoromethyl-phenyl)-urea | HCID 46701839 | 86% |
反応手順
3-(7-Pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenylamine (52 mg, 0.177 mmol) was dissolved in dry DCM under nitrogen atmosphere. p-trifluoromethyl-phenylisocyanate (0.030 mL, 0.212 mmol, 1.2 eq) was added and the mixture was stirred at room temperature for 1 hour and then concentrated under reduced pressure. The crude product was purified by silica gel chromatography (eluant: DCM/MeOH 96:4) to give 73 mg (86%) of 1-[3-(7-pyridin-4-yl-2,3-dihydro-pyrazolo[5,1-b]thiazol-6-yl)-phenyl]-3-(4-trifluoromethyl-phenyl)-urea as white powder.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08524707B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-0e65754bd1f1454ba2cce71666e44790 |
| 出典メモ | uspto-grants-2013_09 |