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HRID 1465992作成日:2026年10月26日

Hydrochloric Acid → 2-(3-Azabicyclo[2.2.2]oct-3-yl)-N-(6-bromo-1-benzothien-2-yl)acetamide hydrochloride

https://huagongshe.com/reaction/1465992

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Carbonate IonHCID 19660—
反応物6-Bromobenzo[b]thiophen-2-amineHCID 17979823—
反応物Pentafluorophenyl (1-azabicyclo[2.2.2]oct-3-yl)acetate hydrochlorideHCID 86610796—
溶媒DimethylformamideHCID 6228—
溶媒AcetonitrileHCID 6342—
生成物2-(3-Azabicyclo[2.2.2]oct-3-yl)-N-(6-bromo-1-benzothien-2-yl)acetamide hydrochlorideHCID 86705776—

反応手順

89.2 mg (0.24 mmol) of pentafluorophenyl (1-azabicyclo[2.2.2]oct-3-yl)acetate hydrochloride are dissolved in 1 ml of DMF, mixed with 71.2 mg (0.31 mmol) of 6-bromo-1-benzothiophene-2-amine and stirred at room temperature overnight. 1 g of MP-carbonate (polymer-bound carbonate, capacity: 2.5-3.5 mmol/g; from Argonaut Technologies, USA) is added. After 3 h, the polystyrene resin is filtered off and washed with THF. The combined filtrates are concentrated in vacuo, and the crude product is purified by preparative HPLC. The hydrochloride is prepared by mixing the product with a mixture of 1 M hydrochloric acid and acetonitrile and again concentrating. Drying under high vacuum results in 14 mg (14% of theory) of the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09000008B2
出典データセットuspto-grants-2015_04
ORD IDord-25b5c426f6b44148a887d9d05fd69497
出典メモuspto-grants-2015_04