1, 3‐Dipolar Cycloaddition of Imidazole Derivatives with Nitrile Oxide: Synthesis of Imidazo[1, 2, 4]oxadiazole Derivatives. Issue 11 (16th August 2017)

• Record Type: Journal Article
• Authors: Jiang, Kun‐Ming; Zhang, Jian‐Qiang; Jin, Yi; Lin, Jun
• Is Part Of: Asian journal of organic chemistry. Volume 6:Issue 11(2017)
• Page Start: 1620
• Page End: 1627
• Publication Date: 2017-08-16
• Subjects: cycloaddition -- cytotoxicity -- density functional calculations -- fused-ring systems -- heterocycles; Chemistry, Organic -- Periodicals; Organic compounds -- Synthesis -- Periodicals; 547.005
• DOI: 10.1002/ajoc.201700347
• Languages: English
• ISSNs: 2193-5807

Abstract

Abstract: A concise and efficient synthesis of imidazo[1, 2, 4]oxadiazole derivatives that proceeds through the [3+2] cycloaddition of 2‐chloro‐1 H ‐benzo[ d ]imidazole with nitrile oxides has been developed. This strategy can conveniently construct tricyclic imidazole heterocyclic derivatives that contain a broad range of functional groups. Compound3 p showed excellent cytotoxic activity against the KYSE410 cell line (IC50 =0.26 μm ). These tricyclic imidazole heterocyclic derivatives are promising candidates for drug discovery. Abstract : Polar express : A concise and efficient synthesis of imidazo[1, 2, 4]oxadiazole derivatives that proceeds through the [3+2] cycloaddition of 2‐chloro‐1 H ‐benzo[d]imidazole with nitrile oxides has been developed. This strategy can be used to conveniently construct tricyclic imidazole heterocyclic derivatives that have a broad range of functional groups. Compound3 p showed excellent cytotoxic activity against the KYSE410 cell line (IC50 =0.26 μm ).