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Methanesulfonyl chloride → N-Cyclopropyl-6-methyl-4'-(5-{[(methylsulfonyl)amino]methyl}-1,3,4-oxadiazol-2-yl)-1,1'-biphenyl-3-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Methanesulfonyl chloride | HCID 31297 | — |
| 反応物 | 4'-[5-(aminomethyl)-1,3,4-oxadiazol-2-yl]-N-cyclopropyl-6-methyl-1,1'-biphenyl-3-carboxamide | HCID 9997891 | — |
| 溶媒 | Pyridine | HCID 1049 | — |
| 生成物 | N-Cyclopropyl-6-methyl-4'-(5-{[(methylsulfonyl)amino]methyl}-1,3,4-oxadiazol-2-yl)-1,1'-biphenyl-3-carboxamide | HCID 10432605 | — |
反応手順
4′-[5-Aminomethyl)-1,3,4-oxadiazol-2-yl]-N-cyclopropyl-6-methyl-1,1′-biphenyl-3-carboxamide (Example 53) (30 mg) was mixed with methanesulphonyl chloride (0.02 ml) and pyridine (0.034 ml) in DCm (3 ml) and the reaction stirred at room temperature for 18 hours. The reaction was washed with water (4×4 ml) and then hydrochloric acid (2N, 5 ml). The organic phase was reduced to dryness under vacuum and the residue purified by HPLC to give after evaporation of the solvents N-cyclopropyl-6-methyl-4′-5-{[(methylsulfonyl)amino]methyl}-1,3,4-oxadiazol-2-yl)-1,1′-biphenyl-3-carboxamide.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07425555B2 |
| 出典データセット | uspto-grants-2008_09 |
| ORD ID | ord-918159baa109468d9773913af6c80e67 |
| 出典メモ | uspto-grants-2008_09 |