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Cesium carbonate → HCID 67258000、化合物
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | 2-(4-Fluorophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane | HCID 2760593 | — |
| 反応物 | HCID 67258967 | HCID 67258967 | — |
| 触媒 | Dichlorobis(tricyclohexylphosphine)pallium (II) | HCID 11050900 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | HCID 67258000 | HCID 67258000 | — |
反応手順
Tert-butyl 4-{6-bromo-1-[(3-ethyl-1,2,4-oxadiazol-5-yl)methyl]-2,4-dioxo-1,4-dihydrothieno[3,2-d]pyrimidin-3(2H)-yl}piperidine-1-carboxylate (500 mg, compound B99), 2-(4-fluorophenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane (246 mg), dichlorobis(tricyclohexylphosphine)palladium (68 mg) and aqueous cesium carbonate solution (0.694 ml, 2.0 M) in dioxane (18 ml) are reacted according to the procedure described in example B55 to afford the title compound after purification by flash column chromatography [silica gel, elution gradient: DCM/EtOH, 100/0 to 70/30 (v/v)] as a solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09018175B2 |
| 出典データセット | uspto-grants-2015_04 |
| ORD ID | ord-e4d8066f9ace4a9db4f523e27bbde9b4 |
| 出典メモ | uspto-grants-2015_04 |