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HRID 1716607作成日:2026年10月25日

Methylorthoformate → 6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazole

https://huagongshe.com/reaction/1716607

反応式

関与物質

役割名称HCID仕込み量
反応物MethylorthoformateHCID 53629101—
反応物4-(2-Amino-5-fluoro-4-methyl-phenylamino)piperidine-1-carboxylic acid tert-butyl esterHCID 58852287—
溶媒Formic AcidHCID 284—
生成物6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazoleHCID 5885230999%

反応条件

温度60 °C

反応手順

To a solution of 4-(2-amino-5-fluoro-4-methyl-phenylamino)piperidine-1-carboxylic acid tert-butyl ester (250 mg, 0.309 mmol) in formic acid (3 mL) was added methyl orthoformate (0.5 mL). After heating for 3 hours at 60° C., the volatiles was removed under reduced pressure to afford crude product 6-fluoro-5-methyl-1-piperidin-4-yl-1H-benzoimidazole (180 mg, 99%) as a brown solid.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07803816B2
出典データセットuspto-grants-2010_09
ORD IDord-4a032e76b0244c44abc2b804fd1ca7a7
出典メモuspto-grants-2010_09