化工社化工社 化学情報印刷レポート · 研究参考用
HRID 421932作成日：2026年10月27日
1,2-Dichloroethane → Tert-butyl{2-[[(7r)-11-({[(3-chloropropyl)sulfonyl]amino}carbonyl)-14-cyclohexyl-7,8-dihydro-6h-indolo[1,2-e][1,5]benzoxazocin-7-yl](methyl)amino]ethyl}carbamate
https://huagongshe.com/reaction/421932
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | 1,2-Dichloroethane | HCID 11 | — |
| 反応物 | 3-Chloropropane-1-sulfonamide | HCID 13614818 | — |
| 反応物 | (7R)-7-[{2-[(tert-butoxycarbonyl)amino]ethyl}(methyl)amino]-14-cyclohexyl-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid | HCID 66674687 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | Tert-butyl{2-[[(7r)-11-({[(3-chloropropyl)sulfonyl]amino}carbonyl)-14-cyclohexyl-7,8-dihydro-6h-indolo[1,2-e][1,5]benzoxazocin-7-yl](methyl)amino]ethyl}carbamate | HCID 86622849 | — |
反応手順
3-chloropropane-1-sulfonamide (1.8 eq), DMAP (2.9 eq) and EDC (1.8 eq), were added to a solution of (7R)-7-[{2-[(tert-butoxycarbonyl)amino]ethyl}(methyl)amino]-14-cyclohexyl-7,8-dihydro-6H-indolo[1,2-e][1,5]benzoxazocine-11-carboxylic acid (prepared as described in Example 1, Step 7) (0.025 M) in DCM. The reaction was stirred under N2 at 40° C. for 2 h, before being allowed to cool. Volatiles were removed in vacuo to leave the crude product as a yellow gum which could be taken on without further purification. (ES+) m/z 687 (M+H)+; 689 (M+H)+
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08101595B2 |
|---|
| 出典データセット | uspto-grants-2012_01 |
|---|
| ORD ID | ord-dd02d376464e4968b8a6dd21f3bd5c29 |
|---|
| 出典メモ | uspto-grants-2012_01 |
|---|
