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HRID 535442作成日:2026年10月26日

Triethylamine → Methyl 2-({[2-(dimethylamino)-2-oxoethyl]carbamoyl}amino)-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoate

https://huagongshe.com/reaction/535442

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物TriphosgeneHCID 94429—
反応物2-Amino-N,N-dimethylacetamide acetateHCID 53399009—
反応物Methyl 2-amino-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoateHCID 66653263—
溶媒WaterHCID 962—
溶媒1,4-DioxaneHCID 31275—
生成物Methyl 2-({[2-(dimethylamino)-2-oxoethyl]carbamoyl}amino)-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoateHCID 66652958143.4%

反応手順

0.798 g (2.69 mmol) of triphosgene diluted in 10 ml of dioxane is added, under an inert atmosphere at ambient temperature, to 1.3 g (3.84 mmol) of methyl 2-amino-5-[(1-methoxy-2-methylindolizin-3-yl)carbonyl]benzoate in 50 ml of dioxane. After stirring for 1 hour, 1.25 g (7.68 mmol) of N,N-dimethylglycinamide acetate and 2.68 ml (19.21 mmol) of triethylamine are added. The reaction medium is stirred overnight at ambient temperature and then hydrolysed with water. The aqueous phase is extracted with dichloromethane. The organic phase obtained is dried over sodium sulphate, filtered, and then concentrated under reduced pressure. 1.8 g of a yellow solid are obtained.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08859544B2
出典データセットuspto-grants-2014_10
ORD IDord-7fe39e2e149f470199cb02595e447c39
出典メモuspto-grants-2014_10