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Water → 8-(cyclohexylmethoxy)-2-methyl-N-[(1R)-2-(methylamino)-1-phenylethyl]imidazo[1,2-a]pyridine-3-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Water | HCID 962 | — |
| 反応物 | 4-Methylbenzenethiol | HCID 7811 | — |
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | 8-(cyclohexylmethoxy)-2-methyl-N-[(1R)-2-{methyl[(2-nitrophenyl)sulfonyl]amino}-1-phenylethyl]imidazo[1,2-a]pyridine-3-carboxamide | HCID 86713513 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Chloroform methanol | HCID 21584188 | — |
| 生成物 | 8-(cyclohexylmethoxy)-2-methyl-N-[(1R)-2-(methylamino)-1-phenylethyl]imidazo[1,2-a]pyridine-3-carboxamide | HCID 86713512 | 57.6% |
反応手順
To a solution of 200 mg of 8-(cyclohexylmethoxy)-2-methyl-N-[(1R)-2-{methyl[(2-nitrophenyl)sulfonyl]amino}-1-phenylethyl]imidazo[1,2-a]pyridine-3-carboxamide in 3 ml of DMF were added 140 mg of potassium carbonate and 50 mg of 4-methylbenzenethiol, followed by stirring for 3 hours. To the reaction mixture were added water and chloroform/methanol (9/1) to carry out a layer separation operation. The organic layer was washed with saturated brine and dried over anhydrous magnesium sulfate, and the solvent was evaporated under reduced pressure. The obtained residue was purified by silica gel column chromatography to obtain 80 mg of 8-(cyclohexylmethoxy)-2-methyl-N-[(1R)-2-(methylamino)-1-phenylethyl]imidazo[1,2-a]pyridine-3-carboxamide.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US09447090B2 |
| 出典データセット | uspto-grants-2016_09 |
| ORD ID | ord-d71a4acd9ada45b696e2cdde6d35b19c |
| 出典メモ | uspto-grants-2016_09 |