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HRID 58694作成日:2026年10月24日

Diisopropylethylamine → N-(2-(6-fluoro-1H-indol-3-yl)ethyl)-5-(3-fluorobenzyl)isoxazole-3-carboxamide

https://huagongshe.com/ja/reaction/58694

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylethylamineHCID 81531—
反応物2-(6-fluoro-1H-indol-3-yl)ethanamineHCID 854024—
反応物Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 9886157—
反応物5-(3-Fluorobenzyl)isoxazole-3-carboxylic acidHCID 66832107—
溶媒DimethylformamideHCID 6228—
生成物N-(2-(6-fluoro-1H-indol-3-yl)ethyl)-5-(3-fluorobenzyl)isoxazole-3-carboxamideHCID 6683176041%

反応手順

A mixture of the 5-(3-fluorobenzyl)isoxazole-3-carboxylic acid (0.057 g; 0.257 mmol), 2-(6-fluoro-1H-indol-3-yl)ethanamine (0.051 g; 0.284 mmol), HATU (0.108 g; 0.284 mmol) and N,N-diisopropylethylamine (0.112 mL; 0.649 mmol) in DMF (3 mL), was stirred at room temperature overnight. The reaction mixture was partitioned between ethyl acetate and sodium hydrogen sulfate, the organic layer was washed with sodium carbonate, brine, dried and concentrated under reduced pressure. The crude mixture was purified by flash chromatography on silica (eluent 20 to 100% ethyl acetate in heptane) to yield 0.040 g (41%) of the title compound as a white solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09434722B2
出典データセットuspto-grants-2016_09
ORD IDord-9298647cc310416583ecc891d6960b78
出典メモuspto-grants-2016_09