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4-Methylmorpholine → 4-[2-(N-BOC-Amino)ethyloxy]benzoyl-2(S)-phenylsulfonylamino-beta-alanine tert-butyl ester
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-Methylmorpholine | HCID 7972 | — |
| 反応物 | Benzotriazol-1-yloxy-tris(dimethylamino)phosphonium hexafluorophosphate | HCID 151348 | — |
| 反応物 | 4-(2-((tert-Butoxycarbonyl)amino)ethoxy)benzoic acid | HCID 2755997 | — |
| 反応物 | (S)-3-amino-2-benzenesulfonylamino-propionic acid tert-butyl ester hydrochloride | HCID 22853534 | — |
| 溶媒 | Acetonitrile | HCID 6342 | — |
| 溶媒 | Ethyl Acetate | HCID 8857 | — |
| 生成物 | 4-[2-(N-BOC-Amino)ethyloxy]benzoyl-2(S)-phenylsulfonylamino-beta-alanine tert-butyl ester | HCID 10840664 | — |
反応手順
To a stirred solution of 1-4 (200 mg, 0.71 mmol), 2-1 (260 mg, 0.85 mmol), NMM (313 μL, 2.8 mmol), and CH3CN (4 mL) at ambient temperature was added BOP reagent (473 mg, 1.1 mmol). After 20 h the reaction mixture was diluted with EtOAc and then washed with H2O, sat. NaHCO3, 10% KHSO4 and brine, dried (MgSO4) and concentrated. Flash chromatography (silica, 40% EtOAc/hexanes) gave 2-3 as a white solid. Rf 0.19 (silica, 40% EtOAc/hexanes).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05929120 |
| 出典データセット | uspto-grants-1999_07 |
| ORD ID | ord-0add4dc143fe4a60a8bbfc141f06ff7b |
| 出典メモ | uspto-grants-1999_07 |