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Hexane → (RS)-S-[3-({[4-(Cyclopropylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)-phenyl]-N-(ethoxycarbonyl)-S-methylsulphoximide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Hexane | HCID 8058 | — |
| 反応物 | Cyclopropylamine | HCID 69828 | — |
| 反応物 | Dichloromethane methanol | HCID 21226129 | — |
| 反応物 | N'-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide | HCID 57788001 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | (RS)-S-[3-({[4-(Cyclopropylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)-phenyl]-N-(ethoxycarbonyl)-S-methylsulphoximide | HCID 57787997 | 68% |
反応手順
According to GWP 5, reaction of N′-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide (72 mg, 0.16 mmol) with cyclopropylamine (13 μL, 0.19 mmol) and chromatographic purification (silica gel, amino column, hexane, dichloromethane/methanol: 0→5% methanol) gives the desired product in 68% yield (50 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07863283B2 |
| 出典データセット | uspto-grants-2011_01 |
| ORD ID | ord-66fdb14fba524afabd69e68ed2222a9f |
| 出典メモ | uspto-grants-2011_01 |