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HRID 41715作成日:2026年10月25日

Dichloromethane → 4-[5-(4-(cyclopropylsulphonyl)piperazin-1-yl)pyridin-2-yl]-3,4-dihydro-2H-quinoxaline-1-carboxylic acid tert-butyl ester

https://huagongshe.com/reaction/41715

反応式

関与物質

役割名称HCID仕込み量
反応物DichloromethaneHCID 6344—
反応物Cyclopropanesulfonyl chlorideHCID 2760919—
反応物4-(5-(piperazin-1-yl)pyridin-2-yl)-3,4-dihydro-2H-quinoxaline-1-carboxylic acid tert-butyl esterHCID 66863782—
溶媒TriethylamineHCID 8471—
生成物4-[5-(4-(cyclopropylsulphonyl)piperazin-1-yl)pyridin-2-yl]-3,4-dihydro-2H-quinoxaline-1-carboxylic acid tert-butyl esterHCID 66863921—

反応手順

10 g of 4-(5-(piperazin-1-yl)pyridin-2-yl)-3,4-dihydro-2H-quinoxaline-1-carboxylic acid tert-butyl ester are placed in a 500 ml round-bottomed flask. 126 ml of dichloromethane are added, followed by 4.23 ml of triethylamine and, finally, 2.7 ml of cyclopropylsulphonyl chloride. The reaction mixture is stirred at ambient temperature for 16 h, then washed with water and once with a saturated sodium chloride solution, dried over magnesium sulphate and then evaporated under reduced pressure. The crude product obtained is chromatographed on silica gel, elution being carried out with a gradient of methanol in dichloromethane varying from 0% to 10%. 10.9 g of 4-[5-(4-(cyclopropylsulphonyl)piperazin-1-yl)pyridin-2-yl]-3,4-dihydro-2H-quinoxaline-1-carboxylic acid tert-butyl ester are obtained.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08530657B2
出典データセットuspto-grants-2013_09
ORD IDord-6d89196070f8439cb3b5da111f665d58
出典メモuspto-grants-2013_09