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HRID 38891作成日:2026年10月26日

Hydrochloric Acid → N-[5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3,4-oxadiazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]-2-(methyloxy)benzenesulfonamide

https://huagongshe.com/reaction/38891

反応式

関与物質

役割名称HCID仕込み量
反応物Hydrochloric AcidHCID 313—
反応物PyridineHCID 1049—
反応物Sodium HydroxideHCID 14798—
反応物2-Methoxybenzenesulfonyl ChlorideHCID 3745851—
反応物5-{4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3,4-oxadiazol-2-yl)-1-[(4-methyl phenyl)sulfonyl]-1H-indazol-6-yl}-2-(methyloxy)-3-pyridinamineHCID 66693613—
溶媒ChloroformHCID 6212—
溶媒1,4-DioxaneHCID 31275—
生成物N-[5-[4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3,4-oxadiazol-2-yl)-1H-indazol-6-yl]-2-(methyloxy)-3-pyridinyl]-2-(methyloxy)benzenesulfonamideHCID 6669133139%

反応手順

5-{4-(5-{[(2R,6S)-2,6-Dimethyl-4-morpholinyl]methyl}-1,3,4-oxadiazol-2-yl)-1-[(4-methylphenyl)sulfonyl]-1H-indazol-6-yl}-2-(methyloxy)-3-pyridinamine (150 mg, 0.254 mmol) was dissolved in chloroform (3 ml) then 2-(methyloxy)benzenesulfonyl chloride (79 mg, 0.382 mmol) was added. Pyridine (0.082 ml, 1.018 mmol) was added to the reaction mixture and it was stirred at room temperature for 5 h. The compound was dissolved in 1,4-dioxane (2 ml) and 2M sodium hydroxide (2 ml) and stirred at room temperature for 3 h. The reaction mixture was neutralized to pH 7 with 2M HCl, then the solvent was removed under a stream of nitrogen. The solid was dissolved in DMSO then filtered through a filter tube and purified by Mass Directed Automated Preparative HPLC. The solvent was removed under nitrogen to give the title compound as a white solid (60 mg).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08524751B2
出典データセットuspto-grants-2013_09
ORD IDord-806177adaf7443e9a48a684cd7ac6adb
出典メモuspto-grants-2013_09