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5-Methylthiophene-2-carboxylic acid → 5-Methyl-thiophene-2-carboxylic acid [2-(1-isopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-Methylthiophene-2-carboxylic acid | HCID 74713 | — |
| 反応物 | 2-Amino-ethanesulfonic acid (1-isopropyl-piperidin-4-yl)-amide | HCID 66624631 | — |
| 生成物 | 5-Methyl-thiophene-2-carboxylic acid [2-(1-isopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide | HCID 66624464 | — |
反応手順
5-Methyl-thiophene-2-carboxylic acid [2-(1-isopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide was prepared by an analogous procedure as described in example 9 starting from 94 mg (1.1 equiv.) 5-methyl-thiophene-2-carboxylic acid and 150 mg (0.60 mmol) 2-amino-ethanesulfonic acid (1-isopropyl-piperidin-4-yl)-amide. Final purification by preparative RP-HPLC (CH3CN/H2O gradient+0.1% TFA) gave pure 5-methyl-thiophene-2-carboxylic acid [2-(1-isopropyl-piperidin-4-ylsulfamoyl)-ethyl]-amide. The title compound was obtained as its trifluoroacetate in form of a colorless amorphous material, which turned out to be hygroscopic with time.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08088925B2 |
| 出典データセット | uspto-grants-2012_01 |
| ORD ID | ord-8a1d35f952b74d96a2ff004b3b23c558 |
| 出典メモ | uspto-grants-2012_01 |