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Sodium Carbonate → N-(Cyclopropylmethyl)-4-methyl-3-(3-piperidin-4-yl-1,2-benzisoxazol-6-yl)benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Sodium Carbonate | HCID 10340 | — |
| 反応物 | N-cyclopropylmethyl-4-methyl-3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzamide | HCID 21914588 | — |
| 反応物 | 6-Bromo-3-piperidin-4-yl-1,2-benzisoxazole | HCID 54121991 | — |
| 触媒 | Tetrakis(triphenylphosphine)palladium | HCID 11979704 | — |
| 溶媒 | 1,2-Dimethoxyethane | HCID 8071 | — |
| 生成物 | N-(Cyclopropylmethyl)-4-methyl-3-(3-piperidin-4-yl-1,2-benzisoxazol-6-yl)benzamide | HCID 10475463 | 50.3% |
反応手順
N-Cyclopropylmethyl-4-methyl-3-(4,4,5,5-tetramethyl-[1,3,2]dioxaborolan-2-yl)-benzamide (Intermediate 21, 100 mg), DME (5 ml), aqueous sodium carbonate (1M, 3 ml), tetrakis (triphenylphosphine) palladium (0) (37 mg) and 6-bromo-3-piperidin-4-yl-1,2-benzisoxazole (76 mg) were heated together at 80° C. under nitrogen for 18 h. The solvent was evaporated and the residue was purified by column chromatography on silica (10 g ) eluting with dichloromethane:ethanol:ammonia (100:8:1 to 70:8:1) to give the title compound (53 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07642276B2 |
| 出典データセット | uspto-grants-2010_01 |
| ORD ID | ord-55d5320b95d54299b2324b117356e3b5 |
| 出典メモ | uspto-grants-2010_01 |