AI Article Synopsis
- A library of anilinoanthraquinone derivatives was created through a parallel Ullmann coupling reaction between bromaminic acid and various aniline derivatives using a compact synthesizer.
- The synthesized products were purified using HPLC and tested for their effectiveness as antagonists of mouse and human P2Y2 receptors.
- Among these, the compound 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716) was identified as a potent P2Y2 antagonist, demonstrating IC50 values in the low micromolar range.
Article Abstract
A library of anilinoanthraquinone derivatives was synthesized by parallel Ullmann coupling reaction of bromaminic acid with aniline derivatives in solution using a compact parallel synthesizer. The products were purified by HPLC and evaluated as antagonists at mouse and human P2Y2 receptors. 4-Phenylamino-substituted 1-amino-2-sulfoanthraquinones, for example, 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716), were potent P2Y2 antagonists with IC50 values in the low micromolar range.
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| http://dx.doi.org/10.1016/j.bmcl.2007.10.082 | DOI Listing |
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Article Synopsis
- A library of anilinoanthraquinone derivatives was created through a parallel Ullmann coupling reaction between bromaminic acid and various aniline derivatives using a compact synthesizer.
- The synthesized products were purified using HPLC and tested for their effectiveness as antagonists of mouse and human P2Y2 receptors.
- Among these, the compound 1-amino-4-(2-methoxyphenyl)-2-sulfoanthraquinone (PSB-716) was identified as a potent P2Y2 antagonist, demonstrating IC50 values in the low micromolar range.
Rapid and efficient microwave-assisted copper(0)-catalyzed ullmann coupling reaction: general access to anilinoanthraquinone derivatives.
Org Lett
March 2007
Pharmaceutical Institute, University of Bonn, D-53121 Bonn, Germany.
[structure: see text]. The synthesis of anilinoanthraquinones 3a-z was achieved by a new, Cu(0)-catalyzed, microwave-assisted Ullmann coupling reaction of bromaminic acid (1) with aniline derivatives 2a-z in phosphate buffer. Good to excellent isolated yields were obtained within only 2-20 min at 80-120 degrees C and 40-100 W.
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