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Potassium Carbonate → 1,1-dimethylethyl 4-[4-[[methyl[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]methyl]-2-thiazolyl]-1-piperidinecarboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Potassium Carbonate | HCID 11430 | — |
| 反応物 | (R)-N-Methyl-1,2,3,4-tetrahydronaphthalen-1-amine | HCID 7128544 | — |
| 反応物 | Tert-butyl 4-[4-(chloromethyl)-1,3-thiazol-2-yl]piperidine-1-carboxylate | HCID 57423790 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 生成物 | 1,1-dimethylethyl 4-[4-[[methyl[(1R)-1,2,3,4-tetrahydro-1-naphthalenyl]amino]methyl]-2-thiazolyl]-1-piperidinecarboxylate | HCID 68527354 | — |
反応手順
A mixture of 1-(1,1-dimethylethyl) 4-(4-chloromethyl-2-thiazolyl)-1-piperidinecarboxylate (i.e. the product of Example 1, Step C) (0.15 g, 0.47 mmol), (1R)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine (0.076 g, 0.47 mmol) and potassium carbonate (0.072 g, 0.52 mmol) in dry acetonitrile (5 mL) was heated at reflux for two days. Then the reaction mixture was filtered, concentrated under reduced pressure, diluted with dichloromethane, and washed with 1 N aqueous hydrochloric acid and water. The organic layers were dried (MgSO4) and concentrated under reduced pressure to give 0.19 g of the title compound as a tan foam.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08084468B2 |
| 出典データセット | uspto-grants-2011_12 |
| ORD ID | ord-cdc1afbb831c4d3ab017758a5d2e8ed3 |
| 出典メモ | uspto-grants-2011_12 |