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Potassium Iodide → 7-Chloro-5-(methylthio)-2-(morpholin-4-ylmethyl)imidazo[1,2-c]pyrimidine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Iodide | HCID 4875 | — |
| 反応物 | Morpholine | HCID 8083 | — |
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | 7-Chloro-2-(chloromethyl)-5-methylsulfanyl-imidazo[1,2-c]pyrimidine | HCID 59299232 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 7-Chloro-5-(methylthio)-2-(morpholin-4-ylmethyl)imidazo[1,2-c]pyrimidine | HCID 59312966 | — |
反応手順
158 mg (1.81 mmol) of morpholine are introduced into 10 ml of DMF at 0° C., and 367 mg (3.63 mmol) of triethylamine and a catalytic amount of potassium iodide are added. A solution of 300 mg of 7-chloro-2-(chloromethyl)-5-(methylthio)imidazo[1,2-c]pyrimidine (Example 26A) in DMF is then slowly added dropwise. The mixture is allowed to reach RT and is stirred at this temperature for a further 16 h. Purification of the crude product by preparative HPLC and drying under high vacuum result in 221.8 mg (41% of theory) of product.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08273752B2 |
| 出典データセット | uspto-grants-2012_09 |
| ORD ID | ord-2b2748f8cfd1441aa27d84c42cd8ea60 |
| 出典メモ | uspto-grants-2012_09 |