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HRID 335607作成日:2026年10月24日

Triethylamine → N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-5-(2-furoylamino)-1-benzothiophene-2-carboxamide hydrochloride

https://huagongshe.com/ja/reaction/335607

反応式

関与物質

役割名称HCID仕込み量
反応物TriethylamineHCID 8471—
反応物2-Furancarbonyl chlorideHCID 68242—
反応物N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-5-amino-1-benzothiophene-2-carboxamide dihydrochlorideHCID 68431067—
溶媒DimethylformamideHCID 6228—
生成物N-[(3R)-1-Azabicyclo[2.2.2]oct-3-yl]-5-(2-furoylamino)-1-benzothiophene-2-carboxamide hydrochlorideHCID 68432467—

反応手順

30 mg (0.08 mmol) of N-[(3R)-1-azabicyclo[2.2.2]oct-3-yl]-5-amino-1-benzo-thiophene-2-carboxamide dihydrochloride are dissolved in 1 ml of DMF, and 33.5 μl (0.24 mmol) of triethylamine are added. At 0° C., 15.7 mg (0.12 mmol) of furan-2-carbonyl chloride are added. After 3 h of stirring at RT, the reaction mixture is separated by preparative HPLC. The product fraction is concentrated under reduced pressure and codistilled with 4M HCl in dioxane. 12 mg (34.7% of theory) of the title compound are obtained.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08884017B2
出典データセットuspto-grants-2014_11
ORD IDord-cb63506461944ca6bc05428ab87c46b5
出典メモuspto-grants-2014_11