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HRID 55774作成日:2026年10月25日

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

https://huagongshe.com/reaction/55774

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-(1-Azabicyclo[2.2.2]oct-3-yl)-N-(6-bromo-1-benzothien-2-yl)acetamide hydrochlorideHCID 17979825—

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US09433614B2
出典データセットuspto-grants-2016_09
ORD IDord-178a4d8d02b44517a92616801e71d0ec
出典メモuspto-grants-2016_09