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N-甲基吗啉 → (S)-2-{(S)-3,3-Dimethyl-2-[(1-methyl-piperidine-4-carbonyl)-amino]-butyrylamino}-propionic acid ethyl ester
参与物
| 角色 | 名称 | HCID | 投料 |
|---|---|---|---|
| 反应物 | N-甲基吗啉 | HCID 7972 | — |
| 反应物 | 氯甲酸异丁酯 | HCID 62365 | — |
| 反应物 | 1-甲基哌啶-4-甲酸 | HCID 2736939 | — |
| 反应物 | (S)-2-((S)-2-Amino-3,3-dimethyl-butyrylamino)-propionic acid ethyl ester | HCID 86674878 | — |
| 溶剂 | N,N-二甲基甲酰胺 | HCID 6228 | — |
| 产物 | (S)-2-{(S)-3,3-Dimethyl-2-[(1-methyl-piperidine-4-carbonyl)-amino]-butyrylamino}-propionic acid ethyl ester | HCID 67325020 | — |
反应步骤
For compound (A48) (S)-2-((S)-2-Amino-3,3-dimethyl-butyrylamino)-propionic acid ethyl ester was coupled with 1-Methyl-piperidine-4-carboxylic acid using isobutylchloroformate and N-methylmorpholine in DMF to give (S)-2-{(S)-3,3-Dimethyl-2-[(1-methyl-piperidine-4-carbonyl)-amino]-butyrylamino}-propionic acid ethyl ester. This was then quaternised with MeI in DCM-acetone and subsequently hydrolysed using an hydroxide resin such as Ambersep 900-OH resin.
来源与证据
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 专利号 | US08541363B2 |
| 来源数据集 | uspto-grants-2013_09 |
| ORD ID | ord-94ce4938ec99444bb640482c7e136ef9 |
| 来源说明 | uspto-grants-2013_09 |