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HRID 4168作成日:2026年10月25日

Triethylamine → 5,11-Dihydro-11-[[(2-propynyl)-amino]carbonyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one

https://huagongshe.com/reaction/4168

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物PropargylamineHCID 239041—
反応物11-chlorocarbonyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-oneHCID 11043962—
溶媒ChloroformHCID 6212—
生成物5,11-Dihydro-11-[[(2-propynyl)-amino]carbonyl]-6H-pyrido[2,3-b][1,4]benzodiazepin-6-oneHCID 20152920—

反応条件

温度40 °C

反応手順

5.5 g (0.1 mol) of propargylamine were added dropwise with stirring at ambient temperature to a suspension of 27.3 g (0.1 mol) of 11-chlorocarbonyl-5,11-dihydro-6H-pyrido[2,3-b][1,4]benzodiazepin-6-one and 10.0 g (0.1 mol) of triethylamine in 500 ml of chloroform, whereupon the temperature rises to 35° C. The mixture is stirred for a further 30 minutes at 40° C., then filtered over activated charcoal and the reaction solution is evaporated to dryness in vacuo. After the oily residue has been decocted with ethyl acetate the desired product is obtained in the form of a colourless crystalline mass in a yield of 20.7 g (71% of theory).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US04724236
出典データセットuspto-grants-1988_02
ORD IDord-da6aacba240a48b7804ec076824d5006
出典メモuspto-grants-1988_02