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HRID 7473作成日:2026年10月25日

Acetic Anhydride → 4-(5-Acetoxy-4-chloro-2-fluoroanilino)-7-benzyloxy-6-methoxycinnoline

https://huagongshe.com/reaction/7473

反応式

関与物質

役割名称HCID仕込み量
反応物Acetic AnhydrideHCID 7918—
反応物7-Benzyloxy-4-(4-chloro-2-fluoro-5-hydroxyanilino)-6-methoxycinnolineHCID 21991047—
触媒4-(Dimethylamino)pyridineHCID 14284—
溶媒PyridineHCID 1049—
生成物4-(5-Acetoxy-4-chloro-2-fluoroanilino)-7-benzyloxy-6-methoxycinnolineHCID 21991032—

反応条件

温度110 °C

反応手順

Acetic anhydride (920 μl, 9.7 mmol) and 4-dimethylaminopyridine (80 mg, 0.65 mmol) were added to a suspension of 7-benzyloxy-4-(4-chloro-2-fluoro-5-hydroxyanilino)-6-methoxycinnoline (3 g, 6.5 mmol), (prepared as described in Example 6), in pyridine (50 ml). After heating at 110° C. for 25 minutes, the solid was filtered off, washed with water and ether and dried under vacuum. The solid was suspended in 2M ethereal hydrogen chloride and the volatiles removed by evaporation to give 4-(5-acetoxy-4-chloro-2-fluoroanilino)-7-benzyloxy-6-methoxycinnoline as the hydrochloride salt (yellow solid, 3.1 g, 94%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07087602B2
出典データセットuspto-grants-2006_08
ORD IDord-86f02a2df9b34f72ae5e90ef9abd5f91
出典メモuspto-grants-2006_08