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5-Amino-2-methylpyridine → (RS)-N-(Ethoxycarbonyl)-S-methyl-S-[3-({[4-(2-methyl-5-pyridylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)phenyl]sulphoximide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 5-Amino-2-methylpyridine | HCID 243313 | — |
| 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)-N-(Ethoxycarbonyl)-S-methyl-S-[3-({[4-(2-methyl-5-pyridylamino)-6-methoxyquinazolin-7-yl]oxy}methyl)phenyl]sulphoximide | HCID 57788021 | 36% |
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 5-amino-2-methylpyridine (28 mg, 0.26 mmol) and chromatography (silica gel, dichloromethane/methanol: 4/1) gives the desired product in 36% yield (40 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-bbafe1208a7f4645992b0e381f65f703 |
| 出典メモ | uspto-grants-2011_01 |