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4-Aminopyridine → (RS)-N-(Ethoxycarbonyl)-S-methyl-S-[3-({[6-methoxy-4-(4-pyridylamino)-quinazolin-7-yl]oxy}methyl)phenyl]sulphoximide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-Aminopyridine | HCID 1727 | — |
| 反応物 | Hexane | HCID 8058 | — |
| 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)-N-(Ethoxycarbonyl)-S-methyl-S-[3-({[6-methoxy-4-(4-pyridylamino)-quinazolin-7-yl]oxy}methyl)phenyl]sulphoximide | HCID 57787969 | 34% |
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 (78 mg, 0.12 mmol) with 4-aminopyridine (19 mg, 0.20 mmol) and chromatographic purification (silica gel, amino column, hexane, dichloromethane/methanol: 0→5% methanol) gives the desired product in 34% yield (29 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-b56ba5c07a0a40c78eb7b9b8dd8d2362 |
| 出典メモ | uspto-grants-2011_01 |