関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Methylorthoformate | HCID 53629101 | — |
| 反応物 | 4-(2-Amino-5-fluoro-4-methyl-phenylamino)piperidine-1-carboxylic acid tert-butyl ester | HCID 58852287 | — |
| 溶媒 | Formic Acid | HCID 284 | — |
| 生成物 | 6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazole | HCID 58852309 | 99% |
反応手順
To a solution of 4-(2-amino-5-fluoro-4-methyl-phenylamino)piperidine-1-carboxylic acid tert-butyl ester (250 mg, 0.309 mmol) in formic acid (3 mL) was added methyl orthoformate (0.5 mL). After heating for 3 hours at 60° C., the volatiles was removed under reduced pressure to afford crude product 6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazole (180 mg, 99%) as a brown solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07803816B2 |
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| 出典データセット | uspto-grants-2010_09 |
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| ORD ID | ord-4a032e76b0244c44abc2b804fd1ca7a7 |
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| 出典メモ | uspto-grants-2010_09 |
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