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HRID 12291作成日:2026年10月25日

Imidazole → 4-[1-(2-Dimethylsilanylethoxymethyl)-1H-benzimidazol-2-yl]-6-imidazol-1-yl-2-(2-trimethylsilanylethoxymethyl)-2H-pyridazin-3-one

https://huagongshe.com/reaction/12291

反応式

関与物質

役割名称HCID仕込み量
反応物ImidazoleHCID 795—
反応物6-oxo-1-(2-trimethylsilanylethoxymethyl)-5-[1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzimidazol-2-yl]-1,6-dihydropyridazine-3-boronic acidHCID 68679702—
触媒Cupric acetateHCID 8895—
溶媒WaterHCID 962—
溶媒PyridineHCID 1049—
生成物4-[1-(2-Dimethylsilanylethoxymethyl)-1H-benzimidazol-2-yl]-6-imidazol-1-yl-2-(2-trimethylsilanylethoxymethyl)-2H-pyridazin-3-oneHCID 131728146—

反応条件

温度80 °C

反応手順

100 mg of 6-oxo-1-(2-trimethylsilanylethoxymethyl)-5-[1-(2-trimethylsilanyl-ethoxymethyl)-1H-benzimidazol-2-yl]-1,6-dihydropyridazine-3-boronic acid (example 55), 35.5 mg of copper(II) acetate and 20 mg of imidazole are dissolved in dry pyridine, and the solution is stirred at 80° C. for 3 hours. For workup, it is diluted with 20 ml of water and extracted several times with ethyl acetate, the organic phases are dried using a silica gel cartridge, and the volatile components are distilled off. The crude product is purified by preparative RP-HPLC (0-100% acetonitrile (+0.05% formic acid) in water (+0.05% formic acid)).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07727989B2
出典データセットuspto-grants-2010_06
ORD IDord-0b1e3bb90b464aa88133a65f8742aa21
出典メモuspto-grants-2010_06