関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Trifluoroacetic acid | HCID 6422 | — |
| 反応物 | Methyl 3-amino-2-thiophenecarboxylate | HCID 89652 | — |
| 反応物 | Trifluoroacetamidine | HCID 2776882 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | 2-(Trifluoromethyl)thieno[3,2-d]pyrimidin-4(3H)-one | HCID 135625376 | 27.7% |
反応手順
To a stirring solution of methyl 3-aminothiophene-2-carboxylate (45a, 1.57, 10.0 mmol) in EtOH (10 mL) was added trifluoroacetamidine (2.24 g, 2 eq) and trifluoroacetic acid (1.54 ml, 2 eq). The resulting mixture was heated to 150° C. for 1 hour in microwave reactor. The reaction mixture was cool and filtered to provide 2-(trifluoromethyl)thieno[3,2-d]pyrimidine-4(3H)-one 45b as a solid (0.61 g). 1H NMR (400 MHz, MeOD) δ ppm: 7.49 (d, J=5.29 Hz, 2H), 8.18 (d, J=5.29 Hz, 1H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08530652B2 |
|---|
| 出典データセット | uspto-grants-2013_09 |
|---|
| ORD ID | ord-88166c9d0f1d4e5aa800b48d75bbf0f0 |
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| 出典メモ | uspto-grants-2013_09 |
|---|
