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HRID 625349作成日:2026年10月25日

Potassium Iodide → Tert-butyl 3-(2-(2-(2-((3-((2-(4-((3-(trifluoromethyl)benzyl)carbamoyl)pyridin-2-yl)-4-(piperidin-1-yl)phenyl)-carbamoyl)benzyl)(methyl)amino)ethoxy)ethoxy)ethoxy)propanoate

https://huagongshe.com/reaction/625349

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium IodideHCID 4875—
反応物Potassium CarbonateHCID 11430—
反応物Methylamino-PEG3-t-butyl esterHCID 53662991—
反応物HCID 66586775HCID 66586775—
溶媒DimethylformamideHCID 6228—
生成物Tert-butyl 3-(2-(2-(2-((3-((2-(4-((3-(trifluoromethyl)benzyl)carbamoyl)pyridin-2-yl)-4-(piperidin-1-yl)phenyl)-carbamoyl)benzyl)(methyl)amino)ethoxy)ethoxy)ethoxy)propanoateHCID 66586756—

反応条件

温度70 °C

反応手順

Into a 8-mL round-bottom flask, was placed a solution of tert-butyl 3-(2-(2-(2-(methylamino)ethoxy)ethoxy)ethoxy)propanoate (89.3 mg, 0.31 mmol, 1.00 equiv) in N,N-dimethylformamide (6 mL), potassium carbonate (84.7 mg, 0.61 mmol, 1.99 equiv), potassium iodide (10.2 mg, 0.06 mmol, 0.20 equiv), and N-(3-(trifluoromethyl)benzyl)-2-(2-(3-(bromomethyl)benzamido)-5-(piperidin-1-yl)phenyl)isonicotinamide (200 mg, 0.31 mmol, 1.00 equiv). The resulting solution was stirred overnight at 70° C. The solids were filtered out. The resulting mixture was concentrated under vacuum. The residue was dissolved in 20 mL of dichloromethane. The resulting mixture was washed with 2×20 mL of water. The resulting mixture was washed with 1×20 mL of brine, dried over sodium sulfate, and concentrated under vacuum. This resulted in 264 mg (crude) of product as yellow oil.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US09301951B2
出典データセットuspto-grants-2016_04
ORD IDord-4fa808b04df54eb5b5a321e505d3ae16
出典メモuspto-grants-2016_04