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HRID 40526作成日:2026年10月24日

Sodium hydride → (S)-N-(1-{4-[3-(2-Cyclopropylmethoxy-pyridin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamide

https://huagongshe.com/ja/reaction/40526

反応式

関与物質

役割名称HCID仕込み量
反応物Sodium hydrideHCID 24758—
反応物CyclopropanemethanolHCID 75644—
反応物(S)-N-(1-{4-[3-(2-Fluoro-pyridin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamideHCID 86689013—
溶媒1,4-DioxaneHCID 31275—
生成物(S)-N-(1-{4-[3-(2-Cyclopropylmethoxy-pyridin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamideHCID 86689027—

反応条件

温度130 °C

反応手順

To 55 mg (0.17 mmol) (S)—N-(1-{4-[3-(2-Fluoro-pyridin-4-yloxy)-azetidin-1-yl]-phenyl}-ethyl)-acetamide (XI.1) in 5 mL 1,4-dioxane is added 0.14 mL (1.73 mmol) cyclopropanemethanol. 38 mg (0.95 mmol, 60% suspension in mineral oil) NaH is added and the mixture is stirred for 15 h at 130° C. After concentration in vacuo the residue is purified by chormotography (silica, ethylacetate) to yield the desired product.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08530461B2
出典データセットuspto-grants-2013_09
ORD IDord-a056d0b03c8f4f7e94bd433ec3b60523
出典メモuspto-grants-2013_09