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HRID 1255972作成日:2026年10月25日

Triethylamine → methanesulfonic acid 2-{2-[4-(4,5-Dichloro-2-fluoro-phenylamino)-6-nitro-quinazolin-7-yloxy]-ethoxy}-ethyl ester

https://huagongshe.com/reaction/1255972

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物Methanesulfonyl chlorideHCID 31297—
反応物2-{2-[4-(4,5-Dichloro-2-fluoro-phenylamino)-6-nitro-quinazoline-7-yloxy]-ethoxy}-ethanolHCID 69266955—
溶媒DichloromethaneHCID 6344—
生成物methanesulfonic acid 2-{2-[4-(4,5-Dichloro-2-fluoro-phenylamino)-6-nitro-quinazolin-7-yloxy]-ethoxy}-ethyl esterHCID 86618842101.9%

反応手順

Compound 29a (0.035 gram, 0.076 mmol) was dissolved in dichloromethane (4.3 ml) and triethylamine (0.032 gram, 3.82 mmol) was added to the resulting solution. Methanesulfonyl chloride (MsCl, 0.025 gram, 0.022 mmol) was then added and the resulting mixture was stirred at room temperature for 3 hours. The mixture was thereafter extracted twice with CH2Cl2, washed with brine and dried over sodium sulfate. The crude residue was purified by silica gel column chromatography, using a mixture of 2% methanol in dichloromethane as eluent, to give Compound 32a (0.012 gram, 29% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08461166B2
出典データセットuspto-grants-2013_06
ORD IDord-b82539dee92c4eb18b087b6a469bbbd4
出典メモuspto-grants-2013_06