Application for the Construction of Oxolinic Acid and BQCA

Application for the Construction of Oxolinic Acid and BQCA

    A copper-catalyzed three-component environmentally benign synthetic method has been developed for the synthesis of substituted 4-quinolone derivatives. In recent study, the researchers at Kaohsiung Medical University have developed a series of 4-quinolones. This method has been successfully applied for the synthesis of available oxolinic acid and BQCA drugs. Traditional synthetic methods limited their applicability due to the requirement of crucial starting precursors, harsh reaction conditions, side product formation and utilization of organic solvents. Thus, considering this facts, the scientist Jeh-Jeng Wang and his colleagues reported water mediated three-component green and sustainable protocol from substituted 3‐(2‐halophenyl)‐3‐oxopropanes, aq. NH3, and aldehydes for the synthesis of valuable N-heterocyclic compounds. In addition, the researchers also demonstrated the synthetic practicality and synthetic application of this strategy; a gram scale reaction and late stage modification of designed product performed. The researchers utilized aq. ammonia as a N1 synthon for the construction of 4-quinolones. Moreover, the researchers extended this reaction with formaldehyde, and other functionalities such as -CN, -NO2, -SO2Ar, -COAr and heterocyclic compounds.

Scheme: Synthesis of 4-Quinolone analogues.

This work was published online in Advanced Synthesis & Catalysis the 1st April 2019. The full name of article entitled “Copper‐Catalyzed Synthesis of Substituted 4‐Quinolones using Water as a Benign Reaction Media: Application for the Construction of Oxolinic Acid and BQCA” is available online through the Adv. Synth. Catal. at: https://onlinelibrary.wiley.com/doi/epdf/10.1002/adsc.201900286.

The lead author of this work “Copper‐Catalyzed Synthesis of Substituted 4‐Quinolones using Water as a Benign Reaction Media: Application for the Construction of Oxolinic Acid and BQCA” are Dr. Babasaheb Sopan Gore, Chein-Chung Lee, Jessica Lee and corresponding author include Jeh-Jeng Wang. ( Professor, Department of Medicinal and Applied Chemistry, Kaohsiung Medical University, Taiwan)

This article-“Copper-Catalyzed Synthesis of Substituted 4-Quinolones using Water as a Benign Reaction Media: Application for the Construction of Oxolinic Acid and BQCA” , written by Rept. Author Jeh-Jeng Wang fom Department of Medicinal and Applied Chemistry, is award for Kaohsiung Medical University 2019 Monthly Excellent Paper Award in July.

The contact Information:

Prof. Dr. Jeh-Jeng Wang, Department of Medicinal and Applied Chemistry, Kaohsiung Medical University, No. 100, Shih-Chuan 1st Rd, Sanmin district, Kaohsiung City, 807 (Taiwan), Tel: (886)-7-3121101 Fax: (886)-7-3125339, E-mail: jjwang@kmu.edu.tw

Dr. Babasaheb Sopan Gore, Postdoctoral Fellow, Kaohsiung Medical University,

Tel: (886)-9-68930195, E-mail: gorepranav99@gmail.com