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HRID 127280作成日:2026年10月26日

Sodium Carbonate → 2-[1-(4-Amino-6,7,8-trimethoxy-2-quinazolinyl)-4-piperidinyl]-isoindolin-1-one monohydrochloride

https://huagongshe.com/reaction/127280

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium CarbonateHCID 10340—
反応物2-Chloro-6,7,8-trimethoxyquinazolin-4-amineHCID 3015804—
反応物2-(Piperidin-4-yl)isoindolin-1-oneHCID 15431961—
溶媒DimethylformamideHCID 6228—
生成物2-[1-(4-Amino-6,7,8-trimethoxy-2-quinazolinyl)-4-piperidinyl]-isoindolin-1-one monohydrochlorideHCID 20556249—

反応手順

The mixture of 5.39 g of 4-amino-2-chloro-6,7,8-trimethoxy-quinazoline, 4.32 g of 2-(4-piperidinyl)-isoindolin-1-one, 4.24 g of anhydrous sodium carbonate and 75 ml of dimethylformamide is stirred under nitrogen at 125°-130° for 16 hours. It is filtered, the filtrate evaporated, the residue dissolved in methylene chloride and the solution washed with aqueous sodium bicarbonate. The organic layer is separated, dried, and evaporated. The residue is suspended in refluxing isopropanol and acidified with hydrogen chloride to pH=1. The precipitate formed is filtered off and triturated with warm ethanol to yield the 2-[1-(4-amino-6,7,8-trimethoxy-2-quinazolinyl)-4-piperidinyl]-isoindolin-1-one monohydrochloride melting at 234° (dec.).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US04255429
出典データセットuspto-grants-1981_03
ORD IDord-faf9295f48a842a48eb8a5dd0b9cfae3
出典メモuspto-grants-1981_03