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Azetidine → Ethyl 6-(azetidin-1-ylmethyl)-2-(trifluoromethyl)pyrimidine-4-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Azetidine | HCID 10422 | — |
| 反応物 | Ethyl 6-(bromomethyl)-2-(trifluoromethyl)pyrimidine-4-carboxylate | HCID 58431340 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Ethyl 6-(azetidin-1-ylmethyl)-2-(trifluoromethyl)pyrimidine-4-carboxylate | HCID 58431385 | 61% |
反応手順
Azetidine (0.62 mL, 9.2 mmol, Aldrich) was added to a solution of ethyl 6-(bromomethyl)-2-(trifluoromethyl)pyrimidine-4-carboxylate (1.76 g, 4.16 mmol, prepared in the manner outlined in Example 47, Step A) in methylene chloride (39 mL). and the reaction was stirred for 20 minutes. Solvent was removed in vacuo and the residue was purified by flash chromatography on silica gel, eluting with a gradient from 0-5% MeOH in DCM to afford product (0.74 g, 61%); LCMS (M+H)+: 290.0.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08933085B2 |
| 出典データセット | uspto-grants-2015_01 |
| ORD ID | ord-f787872e370444099d1e4ca11b2bae0a |
| 出典メモ | uspto-grants-2015_01 |