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Ethyl isocyanatoacetate → Ethyl n-{[(1s,2r)-2-{[1-(4-fluorophenyl)-1h-indazole-5-yl]oxy}-1-methyl-2-phenylethyl]carbamoyl}glycinate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ethyl isocyanatoacetate | HCID 76283 | — |
| 反応物 | (alphaS,betaR)-beta-{[1-(4-Fluorophenyl)-1H-indazole-5-yl]oxy}-alpha-methylbenzeneethanamine | HCID 59339817 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Ethyl n-{[(1s,2r)-2-{[1-(4-fluorophenyl)-1h-indazole-5-yl]oxy}-1-methyl-2-phenylethyl]carbamoyl}glycinate | HCID 44594899 | 79.1% |
反応手順
(αS,βR)-β-{[1-(4-Fluorophenyl)-1H-indazole-5-yl]oxy}-α-methylbenzeneethanamine (80 mg, 0.22 mmol), as described in Example 1, is dissolved in 1.42 mL dichloromethane and ethylisocyanatoacetate (28.6 mg, 0.22 mmol) is dropwise added. After stirring for 45 min at r.t. the solvent is removed and the residue purified by chromatography (silicagel, eluents: hexane/ethylacetate). 85.4 mg (78.6%) of the title compound are obtained.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07728030B2 |
| 出典データセット | uspto-grants-2010_06 |
| ORD ID | ord-82aaeec6ede14f6d8c1b69dc920b0408 |
| 出典メモ | uspto-grants-2010_06 |