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Ammonium formate → Ethyl cis(+/-)-[2-(4-amino-3-methoxypiperidin-1-yl)-1,3-thiazol-4-yl]acetate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ammonium formate | HCID 2723923 | — |
| 反応物 | Ethyl cis(+/-)-[2-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-1,3-thiazol-4-yl]acetate | HCID 86648522 | — |
| 触媒 | HCID 178418390 | HCID 178418390 | — |
| 溶媒 | Ethanol | HCID 702 | — |
| 生成物 | Ethyl cis(+/-)-[2-(4-amino-3-methoxypiperidin-1-yl)-1,3-thiazol-4-yl]acetate | HCID 86648523 | — |
反応手順
Ethyl cis(±)-[2-(4-{[(benzyloxy)carbonyl]amino}-3-methoxypiperidin-1-yl)-1,3-thiazol-4-yl]acetate obtained in Example (64c) (124 mg, 0.29 mmol) was dissolved in ethanol (5 mL). A 10% palladium-carbon catalyst (75 mg) and ammonium formate (90 mg, 1.43 mmol) were added, and the mixture was heated under reflux for 15 hours. The reaction solution was filtered through celite. The filtrate was washed with saturated sodium bicarbonate, dried over anhydrous sodium sulfate and then concentrated under reduced pressure. The resulting compound was used for the next reaction without purification.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08536197B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-0538ab89af514a858730dbf798fd0a4d |
| 出典メモ | uspto-grants-2013_09 |