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Diisopropylethylamine → 3-{4-[(6-{[(2R)-2-(3-Fluoro-4-hydroxyphenyl)-2-hydroxyethyl]amino}hexyl)oxy]butyl}benzenesulfonamide formate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Benzenesulfonamide, 3-[4-[(6-bromohexyl)oxy]butyl]- | HCID 21895438 | — |
| 反応物 | 4-[(1R)-2-amino-1-hydroxyethyl]-2-fluorophenol | HCID 68864472 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | 3-{4-[(6-{[(2R)-2-(3-Fluoro-4-hydroxyphenyl)-2-hydroxyethyl]amino}hexyl)oxy]butyl}benzenesulfonamide formate | HCID 69318922 | 62.1% |
反応手順
A stirred solution of 4-[(1R)-2-amino-1-hydroxyethyl]-2-fluorophenol (45 mg), diisopropylethylamine (0.06 ml) and 3-{4-[(6-bromohexyl)oxy]butyl}benzenesulfonamide (86 mg) in N,N-dimethylformamide (1 ml) under nitrogen was heated to 50° for 18 h. The mixture was cooled to 20°, the solvent evaporated in vacuo and the residue purified by mass-directed autopreparative HPLC to give the title compound (36 mg). LCMS RT=2.37 min, ES+ve 483 (MH)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07402598B2 |
| 出典データセット | uspto-grants-2008_07 |
| ORD ID | ord-3703fa36968a4bec8eefa28bfbaf5e55 |
| 出典メモ | uspto-grants-2008_07 |