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HRID 971072作成日:2026年10月25日

1,1'-Carbonyldiimidazole → Pruvanserin

https://huagongshe.com/reaction/971072

反応式

関与物質

役割名称HCID仕込み量
反応物1,1'-CarbonyldiimidazoleHCID 68263—
反応物3-Cyano-1H-indole-7-carboxylic acidHCID 11367431—
反応物1-[2-(4-Fluorophenyl)ethyl]piperazine dihydrochlorideHCID 45158333—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物PruvanserinHCID 6433122—

反応手順

5 g (0.027 mol) of 3-cyanoindole-7-carboxylic acid are dissolved in 40 ml of hot N-methylpyrrolidone, the solution is cooled to 40°, and 7.6 g (0.027 mol) of N,N-carbonyldiimidazole are added. The mixture is stirred at room temperature for a further one hour. A suspension of 1-(2-(4-fluorophenyl)ethyl)piperazine dihydrochloride in 40 ml of N-methylpyrrolidone is subsequently poured in. After 5 minutes, a clear solution is formed and just afterwards white crystals deposit. The mixture is stirred overnight at room temperature. The crystals are filtered off with suction, washed and dried, giving 5 g of 7-{4-[2-(4-fluorophenyl)ethyl]piperazin-1-carbonyl}-1H-indole-3-carbonitrile as the free base having a melting point (m.p.) of 192.0-193.5°.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07312342B2
出典データセットuspto-grants-2007_12
ORD IDord-2164d0cef5b9403696677fdf3ab962de
出典メモuspto-grants-2007_12