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2-Methylbenzenesulfonamide → N-[4-[1-(2-Carbamoylethyl)-5-(N-cyclopentylmethyl carbamoyl)indol-3-ylmethyl]-3-methoxybenzoyl]-2-methylbenzenesulphonamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Methylbenzenesulfonamide | HCID 6924 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | 4[1-(2-Carbamoylethyl)-5-(N-cyclopentylmethylcarbamoyl)indol-3-ylmethyl]-3-methoxybenzoic acid | HCID 19822469 | — |
| 触媒 | 4-(Dimethylamino)pyridine | HCID 14284 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | N-[4-[1-(2-Carbamoylethyl)-5-(N-cyclopentylmethyl carbamoyl)indol-3-ylmethyl]-3-methoxybenzoyl]-2-methylbenzenesulphonamide | HCID 19822468 | 37% |
反応手順
A solution of 4-[1-(2-carbamoylethyl)-5-(N-cyclopentylmethylcarbamoyl)indol-3-ylmethyl]-3-methoxybenzoic acid (77 mg), 4-(dimethylamino)pyridine (20 mg), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (37 mg), and ortho-toluenesulphonamide (28 mg) in dichloromethane (2.0 ml) was stirred under a nitrogen atmosphere for 48 hours. The mixture was diluted with dichloromethane; washed with 10% v/v hydrochloric acid, water, and brine; and evaporated. The resulting white solid was crystallized from ethyl acetate/hexane to give the title compound (37 mg; 37%) as a white solid; mp 140°-145° C. (d).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US04918094 |
| 出典データセット | uspto-grants-1990_04 |
| ORD ID | ord-f4749c91c72744a99289e23ae64dfe3e |
| 出典メモ | uspto-grants-1990_04 |