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4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride → (2R)-N-(4-cyanophenyl)-2-hydroxy-2-[(2R)-3-oxo-4-[4-(3-oxomorpholin-4-yl)phenyl]morpholin-2-yl]acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-(4,6-Dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride | HCID 2734059 | — |
| 反応物 | 2-(2-Chloroethoxy)acetic acid | HCID 10920584 | — |
| 反応物 | (2R)-2-[(2R)-4-(4-aminophenyl)-3-oxomorpholin-2-yl]-N-(4-cyanophenyl)-2-hydroxyacetamide | HCID 67032877 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | (2R)-N-(4-cyanophenyl)-2-hydroxy-2-[(2R)-3-oxo-4-[4-(3-oxomorpholin-4-yl)phenyl]morpholin-2-yl]acetamide | HCID 67222610 | 73.2% |
反応手順
To a suspension of compound 26-5 (0.1 g) and 2-chloroethoxy acetic acid (45.4 mg) in DMF (2 mL), was added 4-(4,6-dimethoxy-1,3,5-triazin-2-yl)-4-methylmorpholinium chloride (DMT-MM; 87.7 mg). The reaction mixture was stirred at room temperature overnight. Then, according to the Step 29-1 in synthetic method for EXAMPLE 29, cyclization reaction was pursued to obtain compound 30-1 (90 mg) as a colorless amorphous solid.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08987242B2 |
| 出典データセット | uspto-grants-2015_03 |
| ORD ID | ord-f31e4ae7ca28494aa4b4a360e89da4d8 |
| 出典メモ | uspto-grants-2015_03 |