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1,2-二氯乙烷 → [2-(2-Amino-3-methoxy-phenylcarbamoyl)-ethyl]-methyl-carbamic acid tert.-butyl ester
参与物
| 角色 | 名称 | HCID | 投料 |
|---|---|---|---|
| 反应物 | 1,2-二氯乙烷 | HCID 11 | — |
| 反应物 | 1-羟基苯并三唑(HOBT) | HCID 75771 | — |
| 反应物 | N,N-二异丙基乙胺 | HCID 81531 | — |
| 反应物 | 1,2-二氨基-3-甲氧基苯 | HCID 184268 | — |
| 反应物 | Tert.-butoxycarbonyl-methylamino-propanoic acid | HCID 86641926 | — |
| 催化剂 | 4-二甲氨基吡啶(DMAP) | HCID 14284 | — |
| 溶剂 | 二氯甲烷 | HCID 6344 | — |
| 产物 | [2-(2-Amino-3-methoxy-phenylcarbamoyl)-ethyl]-methyl-carbamic acid tert.-butyl ester | HCID 68411798 | — |
反应步骤
To a solution of 1.35 g of tert.-butoxycarbonyl-methylamino-propanoic acid in 50 mL DCM were added 3.4 mL of DIPEA, 81 mg of DMAP, 1.0 g of HOBt, 1.5 g of EDC and 0.91 g of 3-methoxybenzene-1,2-diamine. The resulting mixture was stirred at rt for 3 h and then quenched with water. The organic phase was washed with sat. aq. NaHCO3, dried over MgSO4 and concentrated on vacuo to yield 2.9 g of [2-(2-amino-3-methoxy-phenylcarbamoyl)-ethyl]-methyl-carbamic acid tert.-butyl ester as brown oil.
来源与证据
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 专利号 | US08202885B2 |
| 来源数据集 | uspto-grants-2012_06 |
| ORD ID | ord-39e36709953048d28651a2f8cb4122a3 |
| 来源说明 | uspto-grants-2012_06 |