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3-Aminobenzonitrile → (RS)-S-{3-[({4-[(3-Cyanophenyl)amino]-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 | 3-Aminobenzonitrile | HCID 16702 | — |
| 反応物 | N'-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide | HCID 57788001 | — |
| 溶媒 | Dichloromethane methanol | HCID 21226129 | — |
| 生成物 | (RS)-S-{3-[({4-[(3-Cyanophenyl)amino]-6-methoxyquinazolin-7-yl}oxy)methyl]-phenyl}-N-(ethoxycarbonyl)-S-methylsulphoximide | HCID 57788002 | 71% |
反応手順
According to GWP 5, the reaction of N′-(2-cyano-5-{3-[(RS)-N-(ethoxycarbonyl)-S-methylsulphonimidoyl]benzyloxy}-4-methoxyphenyl)-N,N-dimethylformimidamide (100 mg, 0.22 mmol) with 3-aminobenzonitrile (31 mg, 0.26 mmol) and chromatography (silica gel, dichloromethane/methanol: 4/1) gives the desired product in 71% yield (82 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-4abb6b63243e4567b96af808c4e41b96 |
| 出典メモ | uspto-grants-2011_01 |