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4-Methylmorpholine → 4-(N-Boc-N'-Piperazinyl)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-[4-(tert-Butoxycarbonyl)piperazin-1-yl]benzoic acid | HCID 2795508 | — |
| 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-(N-Boc-N'-Piperazinyl)benzoyl-2(S)-phenylsulfonylamino-beta-alanine tert-butyl ester | HCID 86751089 | — |
反応手順
A mixture of 22-4 (300 mg, 1.0 mmol), 19-2a (329 mg, 1.0 mmol), NMM (430 gL, 4.0 mmol), and CH3CN (5 mL) at ambient temperature was treated with BOP (650 mg, 1.5 mmol). After 20 h the reaction mixture was diluted with EtOAc and then washed with 10% KHSO4 and brine, dried (MgSO4) and concentrated. Flash chromatography (silica, 40% EtOAc/hexanes) gave 22-5 as a white solid. TLC Rf =0.16 (silica, 40% EtOAc/hexanes);
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05648368 |
| 出典データセット | uspto-grants-1997_07 |
| ORD ID | ord-eb18c29e59a446ed80c4e3a93787d3ef |
| 出典メモ | uspto-grants-1997_07 |