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4-Methylmorpholine → 3-bromo-N-[(1R)-1-(5-chloro-1H-benzimidazol-2-yl)-2-methoxyethyl]-4-(2,5-dihydropyrrol-1-ylcarbonyl)benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-Methylmorpholine | HCID 7972 | — |
| 反応物 | O-(Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate | HCID 2733207 | — |
| 反応物 | 3-Bromo-4-(2,5-dihydropyrrol-1-ylcarbonyl)benzoic acid | HCID 69309865 | — |
| 反応物 | Bromine chlorine | HCID 131726752 | — |
| 反応物 | HCID 178495727 | HCID 178495727 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 溶媒 | Dichloromethane methanol | HCID 21226129 | — |
| 生成物 | 3-bromo-N-[(1R)-1-(5-chloro-1H-benzimidazol-2-yl)-2-methoxyethyl]-4-(2,5-dihydropyrrol-1-ylcarbonyl)benzamide | HCID 178495734 | 83% |
反応手順
Prepared analogously to Example 1g from 3-bromo-4-(2,5-dihydropyrrol-1-ylcarbonyl)benzoic acid, TBTU, N-methylmorpholine, and (1R)-1-(5-chloro-1H-benzimidazol-2-yl)-2-methoxyethylamine in N,N-dimethylformamide. Yield: 83%; Rf value: 0.41 (silica gel; dichloromethane/methanol=95:5); C22H20BrClN4O3 (503.79); mass spectrum: (M+H)+=503/505/507 (bromine/chlorine isotope).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07326791B2 |
| 出典データセット | uspto-grants-2008_02 |
| ORD ID | ord-56c29bd79e7c404b9a5ddb88d2de9b5f |
| 出典メモ | uspto-grants-2008_02 |