8-Chloro-4-methyl-2-phenyl-3,4-dihydropyrido[3,2-F][1,4]oxazepin-5(2H)-one → 8-[3-Methoxy-4-(4-methylimidazol-1-yl)anilino]-4-methyl-2-phenyl-2,3-dihydropyrido[3,2-f][1,4]oxazepin-5-one

HRID 614

反応式

HRID 614 の反応式
CN1CC(c2ccccc2)Oc2nc(Cl)ccc2C1=O.COc1cc(N)ccc1-n1cnc(C)c1.Cl>CC(=O)O.CC(=O)O.COCCOC.O=C([O-])[O-].[Cs+].[Cs+].[Pd].c1ccc(-c2ccccc2P(C2CCCCC2)C2CCCCC2)cc1>COc1cc(Nc2ccc3c(n2)OC(c2ccccc2)CN(C)C3=O)ccc1-n1cnc(C)c1

参加物

7

反応物 2

HCID 595778258-Chloro-4-methyl-2-phenyl-3,4-dihydropyrido[3,2-F][1,4]oxazepin-5(2H)-oneHCID 674242353-Methoxy-4-(4-methyl-1H-imidazol-1-yl)aniline hydrochloride

生成物 1

HCID 498200868-[3-Methoxy-4-(4-methylimidazol-1-yl)anilino]-4-methyl-2-phenyl-2,3-dihydropyrido[3,2-f][1,4]oxazepin-5-one収率 40.02%

試薬・触媒・溶媒 4

HCID 10796Cesium carbonate試薬HCID 27342162-(Dicyclohexylphosphino)biphenyl触媒HCID 4144353Palladium (II) acetate触媒HCID 80711,2-Dimethoxyethane溶媒

反応条件

温度
100 °C

実験手順

were placed in a microwave vial equipped with a stirring bar. The vial was capped and flushed with argon. DME (2 mL) and Et3N (0.028 mL, 0.20 mmol) were added via a syringe and the mixture was stirred at room temperature for 30 min and then heated to 100°C in a microwave apparatus for 1h. The reaction mixture was diluted with dichloromethane and ethyl acetate, fitered and concentrated. The residue was purified by reversed phase HPLC to give 37 mg of the product as a solid.

出典と根拠

ORDレコード
ord-322a5f0c927a43d5b08115d8443f975d
出典データセット
750 AstraZeneca ELN dataset
元リンク
出典を表示

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