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3-Oxetanone → 6-Chloro-1-[6-[4-(oxetan-3-yl)-1,4-diazepan-1-yl]-2-pyridyl]pyrazolo[4,3-c]pyridine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-Oxetanone | HCID 15024254 | — |
| 反応物 | 6-Chloro-1-[6-(1,4-diazepan-1-yl)-2-pyridyl]pyrazolo[4,3-c]pyridine | HCID 86707050 | — |
| 溶媒 | 1,2-Dichloroethane | HCID 11 | — |
| 生成物 | 6-Chloro-1-[6-[4-(oxetan-3-yl)-1,4-diazepan-1-yl]-2-pyridyl]pyrazolo[4,3-c]pyridine | HCID 86707138 | 63% |
反応手順
A mixture of 6-chloro-1-[6-(1,4-diazepan-1-yl)-2-pyridyl]pyrazolo[4,3-c]pyridine (0.4094 mmol; 134.6 mg), oxetan-3-one (0.4912 mmol; 35.40 mg), and Molecular sieve (4A) in 1,2-dichloroethane (12 ml) was stirred at room temperature for 4 hours. STAB (0.6141 mmol; 137.0 mg) was added. The reaction was stirred for 3 days. The mixture was filtered through Celite. The filtrate was concentrated and the residue was purified on silica eluted with 0 to 5% MeOH in DCM to afford 6-chloro-1-[6-[4-(oxetan-3-yl)-1,4-diazepan-1-yl]-2-pyridyl]pyrazolo[4,3-c]pyridine (99.2 mg, 63%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09434725B2 |
| 出典データセット | uspto-grants-2016_09 |
| ORD ID | ord-6e997d4893474b41b11d9ff12a2b1149 |
| 出典メモ | uspto-grants-2016_09 |