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Lithium Hydroxide → cis(+/-)-2-(3-Chloro-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}piperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Lithium Hydroxide | HCID 3939 | — |
| 反応物 | Ethyl cis(+/-)-2-(3-chloro-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}piperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate | HCID 86648773 | — |
| 生成物 | cis(+/-)-2-(3-Chloro-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}piperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylic acid | HCID 86648774 | 34.2% |
反応手順
The same operation as in Example (2652d) was performed using ethyl cis(±)-2-(3-chloro-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}piperidin-1-yl)-4-methyl-1,3-thiazole-5-carboxylate obtained in Example (198c) (78 mg, 0.169 mmol) and a 2 N aqueous lithium hydroxide solution (848 μL). The resulting pale yellow solid was purified by thin layer silica gel chromatography (eluent: chloroform:tetrahydrofuran=3:2 v/v) to obtain 25 mg of the title compound (34%) as a colorless solid from the more polar elution fraction.
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-b53b820cbdd741f48a0c5af3116986d4 |
| 出典メモ | uspto-grants-2013_09 |