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HRID 347794作成日:2026年10月27日

Diisopropylcarbodiimide → {2-[2-({4-[3-[3-(4-Fluorophenyl)-3-hydroxypropyl]-2-(4-methoxyphenyl)-4-oxoazetidin-1-yl]benzylcarbamoyl}methoxy)ethoxy]ethoxy}acetic acid

https://huagongshe.com/reaction/347794

反応式

関与物質

役割名称HCID仕込み量
反応物DiisopropylcarbodiimideHCID 12734—
反応物3,6,9-Trioxaundecanedioic acidHCID 83793—
反応物1-(4-Aminomethylphenyl)-3-[3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-methoxyphenyl)azetidin-2-oneHCID 12111622—
反応物HCID 178418300HCID 178418300—
溶媒DimethylformamideHCID 6228—
溶媒TriethylamineHCID 8471—
生成物{2-[2-({4-[3-[3-(4-Fluorophenyl)-3-hydroxypropyl]-2-(4-methoxyphenyl)-4-oxoazetidin-1-yl]benzylcarbamoyl}methoxy)ethoxy]ethoxy}acetic acidHCID 21083134—

反応手順

A solution of 64 mg of 1-(4-aminomethylphenyl)-3-[3-(4-fluorophenyl)-3-hydroxypropyl]-4-(4-methoxyphenyl)azetidin-2-one (5), and 21 μl of triethylamine in 1 ml of dimethylformamide was added to a solution of 327 mg of 3,6,9-trioxaundecanedioic acid, 57 μl of diisopropylcarbodiimide, 50 mg of hydroxybenzotriazole in 2 ml of dimethylformamide, and the mixture was stirred at room temperature for 12 h. The reaction solution was concentrated and separated by HPLC (Knauer Eurospher-100-10-C18, water (0.1% trifluoroacetic acid)/acetonitrile (0.1% trifluoroacetic acid)=80/20->10/90). This gave the product of molecular weight 638.70 (C34H39F1N2O9); MS (ESI) 639.27 (M+H+)

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07176193B2
出典データセットuspto-grants-2007_02
ORD IDord-f1c92fd9803744d3b792dd673c25adfc
出典メモuspto-grants-2007_02