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HRID 2201140作成日:2026年10月24日

Ethyl Acetate → (R)-2-(6-chloro-5-cyano-3-fluoropyridin-2-ylamino)butanamide

https://huagongshe.com/ja/reaction/2201140

反応式

関与物質

役割名称HCID仕込み量
反応物Ethyl AcetateHCID 8857—
反応物DiisopropylethylamineHCID 81531—
反応物2,6-Dichloro-5-fluoro-3-pyridinecarbonitrileHCID 2733849—
反応物(2R)-2-aminobutanamide hydrochlorideHCID 16218339—
溶媒N-methyl-2-pyrrolidoneHCID 13387—
生成物(R)-2-(6-chloro-5-cyano-3-fluoropyridin-2-ylamino)butanamideHCID 8666616098.2%

反応手順

To the mixture of (R)-(−)-2-aminobutanamide hydrochloride (1.00 g, 7.2 mmol) and 2,6-dichloro-5-fluoro-3-pyridinecarbonitrile (0.92 g, 4.8 mmol) in 40 mL NMP added DIEA (2.5 mL, 14.4 mmol). The mixture was then sent to 100° C. for stirring for 1 h. The mixture was cooled to RT, and to it was poured 300 mL EtOAc. The mixture was washed with brine four times. The organic phase was dried, concentrated and purified using silica flash column (70% EtOAc-30% DCM) to isolate (R)-2-(6-chloro-5-cyano-3-fluoropyridin-2-ylamino)butanamide (1.21 g, 98% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09359375B2
出典データセットuspto-grants-2016_06
ORD IDord-3e3999361bb6441db89323c44ede302c
出典メモuspto-grants-2016_06