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2-Bromopyrimidine → 2-[3-(1-Pyrimidin-2-ylpiperidin-4-ylmethyl)-[1,2,4]oxadiazol-5-yl]furo[3,2-c]pyridine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Bromopyrimidine | HCID 78345 | — |
| 反応物 | 1,8-Diazabicyclo(5.4.0)undec-7-ene | HCID 81184 | — |
| 反応物 | 2-(3-Piperidin-4-ylmethyl-[1,2,4]oxadiazol-5-yl)furo[3,2-c]pyridine | HCID 11630584 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 2-[3-(1-Pyrimidin-2-ylpiperidin-4-ylmethyl)-[1,2,4]oxadiazol-5-yl]furo[3,2-c]pyridine | HCID 57659445 | — |
反応手順
DBU (53 ΔL, 352 Amos) was added to a stirred solution of 2-(3-piperidin-4-ylmethyl-[1,2,4]oxadiazol-5-yl)furo[3,2-c]pyridine (Preparation 12, 50 mg, 176 μmol) and 2-bromopyrimidine (31 mg, 193 μmol) in dioxane (1 mL) at 20° C. After 2 d, the solvent was removed in vacuo, then the residue was purified by chromatography (MeOH—CH2Cl2, 1:19) to yield the title compound: RT=2.64 min; m/z (ES+)=363.1 [M+H]+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08193359B2 |
| 出典データセット | uspto-grants-2012_06 |
| ORD ID | ord-5dc9b5405800447db90dd76ea6f92d39 |
| 出典メモ | uspto-grants-2012_06 |