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HRID 642982作成日:2026年10月25日

Potassium Carbonate → 5-Chloro-N-((1-(4-(2,4-dimethoxypyrimidin-5-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)thiophene-2-carboxamide

https://huagongshe.com/reaction/642982

反応式

関与物質

役割名称HCID仕込み量
反応物Potassium CarbonateHCID 11430—
反応物(2,4-Dimethoxypyrimidin-5-yl)boronic acidHCID 2736209—
反応物5-chloro-N-((1-(4-iodophenyl)-1H-1,2,3-triazol-4-yl)methyl)thiophene-2-carboxamideHCID 57640693—
触媒HCID 178418476HCID 178418476—
溶媒WaterHCID 962—
溶媒AcetonitrileHCID 6342—
生成物5-Chloro-N-((1-(4-(2,4-dimethoxypyrimidin-5-yl)phenyl)-1H-1,2,3-triazol-4-yl)methyl)thiophene-2-carboxamideHCID 24990944—

反応条件

温度125 °C

反応手順

The mixture of 5-chloro-N-((1-(4-iodophenyl)-1H-1,2,3-triazol-4-yl)methyl)thiophene-2-carboxamide (4.1, 48 mg, 0.11 mmol, synthesized by procedures similar to those that were used to make compound 1.5 described in SCHEME 1), 2,4-dimethoxypyrimidin-5-ylboronic acid (4.2, 24 mg, 0.13 mmol), PdCl2(PPh3)2 (38 mg, 0.05 mmol), K2CO3 (23 mg, 0.16 mmol) in 1 mL acetonitrile and 1 mL water was degassed using argon stream and heated in microwave reactor at 125° C. for 15 min. The mixture was filtered and directly subjected to reverse phase prep HPLC to isolate the title compound. MS found for C20H17ClN6O3S (M+H)+ 457.1, 459.1 (Cl pattern).

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07696352B2
出典データセットuspto-grants-2010_04
ORD IDord-4f70147975714e1fbcb6d2f849feffd0
出典メモuspto-grants-2010_04