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HRID 1162787作成日:2026年10月24日

Formic Acid → 2-(2-(4-(2-(Methylamino)ethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamide

https://huagongshe.com/ja/reaction/1162787

反応式

関与物質

役割名称HCID仕込み量
反応物Formic AcidHCID 284—
反応物MethylamineHCID 6329—
反応物2-(1-(2-(3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)1H-pyrazol-4-yl)ethyl methanesulfonateHCID 59520461—
溶媒DimethylformamideHCID 6228—
生成物2-(2-(4-(2-(Methylamino)ethyl)-3-(trifluoromethyl)-1H-pyrazol-1-yl)acetamido)-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxamideHCID 5952046613.1%

反応条件

温度120 °C

反応手順

The 2-(1-(2-(3-carbamoyl-4,5,6,7-tetrahydrobenzo[b]thiophen-2-ylamino)-2-oxoethyl)-3-(trifluoromethyl)1H-pyrazol-4-yl)ethyl methanesulfonate (30 mg, 0.061 mmol) was dissolved in DMF (1 mL) and methylamine (2 M in THF, 1 mL, 2 mmol) added. The reaction mixture was heated at 120° C. for 5 min in the microwave. The THF was removed in vacuo and the reaction mixture filtered and purified by preparative reverse phase HPLC to give the formic acid salt of the desired product (3.6 mg, 0.008 mmol, 12%).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07820707B2
出典データセットuspto-grants-2010_10
ORD IDord-4fcfae59353649e49cdea4ee85fd3982
出典メモuspto-grants-2010_10