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HRID 11696作成日:2026年10月25日

Triethylamine → N-[3-(3-{2-[4-(4-Fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-6-methyl-pyridin-2-yl)-propionyl]-methanesulfonamide

https://huagongshe.com/reaction/11696

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物MethanesulfonamideHCID 72879—
反応物1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
反応物3-(3-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-6-methyl-pyridin-2-yl)-propionic acidHCID 69655226—
触媒4-(Dimethylamino)pyridineHCID 14284—
溶媒DichloromethaneHCID 6344—
生成物N-[3-(3-{2-[4-(4-Fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-6-methyl-pyridin-2-yl)-propionyl]-methanesulfonamideHCID 6965577942.6%

反応手順

To a solution of 3-(3-{2-[4-(4-fluoro-benzyl)-(2R,5S)-2,5-dimethyl-piperazin-1-yl]-2-oxo-ethoxy}-6-methyl-pyridin-2-yl)-propionic acid (0.10 g, 0.23 mmol) in methylene chloride (2 mL) was added 4-dimethylaminopyridine (0.032 g, 0.27 mmol), (3-(dimethylamino)propyl)ethyl carbodiimide hydrochloride (0.051 g, 0.27 mmol), methanesulfonamide (0.025 g, 0.27 mmol) and triethylamine (0.037 mL, 0.27 mmol). The reaction was stirred at ambient temperature for 18 hours. The reaction mixture was then diluted with dichloromethane and washed with 0.2 M hydrochloric acid. The organic layer was dried over magnesium sulfate, filtered and concentrated in vacuo. The crude product was purified by chromatography on silica gel to give the title compound (0.051 g, LRMS: 521.5).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07098212B2
出典データセットuspto-grants-2006_08
ORD IDord-63c48ff29cef4147bc2af082637a14cc
出典メモuspto-grants-2006_08