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HRID 512978作成日:2026年10月26日

Cyclohexene → N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-amino-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamide

https://huagongshe.com/reaction/512978

反応式

関与物質

役割名称HCID仕込み量
反応物CyclohexeneHCID 8079—
反応物N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-nitro-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamideHCID 86647627—
触媒PalladiumHCID 23938—
溶媒1,4-DioxaneHCID 31275—
生成物N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-amino-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamideHCID 8664762882%

反応条件

温度100 °C

反応手順

A mixture of N-[5-(3,5-difluorobenzyl)-1H-indazol-3-yl]-4-nitro-2-[tetrahydro-2H-pyran-4-yl(trifluoroacetyl)amino]benzamide (3.86 g, 6.4 mmol), cyclohexene (10 mL), dioxane (70 mL) and 10% Pd/C (0.42 g) was stirred at 100° C. for 4 hours. The reaction mixture was filtered over a celite pad washing thoroughly with THF and MeOH. After evaporation of the organic phase, purification of the crude by chromatography over silica gel (DCM/EtOH 9/1) gave 2.75 g of title compound (82% yield).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09102662B2
出典データセットuspto-grants-2015_08
ORD IDord-81c2bf587aea4e6e84516bdab721ca45
出典メモuspto-grants-2015_08