3-(Arylamino)-1,2,4-triazin-5-one: A Novel Synthesis and Its Use

• Published in: European Journal of Organic Chemistry Vol. 2010; no. 15; pp. 2852 - 2854
• Main Authors: Leenders, Ruben, Heeres, Jan, Vandenput, Dirk, Zijlmans, Remco, Guillemont, Jérôme, Lewi, Paul
• Format: Book Review Journal Article
• Language: English
• Published: Weinheim WILEY-VCH Verlag 01.05.2010; WILEY‐VCH Verlag; Wiley; Wiley-VCH
• Subjects: Antiviral agents; Chemistry; Chemistry, Organic; Exact sciences and technology; Heterocyclic compounds; Heterocyclic compounds with several n hetero atoms in the same ring, in separated rings or in fused rings; Medicinal chemistry; Nitrogen heterocycles; Noncondensed benzenic compounds; Organic chemistry; Physical Sciences; Preparations and properties; Science & Technology; Antiviral agents; Medicinal chemistry; Nitrogen heterocycles; 1,2,4-TRIAZINE DERIVATIVES; Functionalization; Nitrogen heterocycle; Triazine derivatives; Phenols; Antiviral; Benzenic compound; Aniline derivatives; Chemical synthesis; Arylamine
• ISSN: 1434-193X; 1099-0690
• DOI: 10.1002/ejoc.201000242

An optimized procedure is given for the synthesis of novel 3‐(arylamino)‐1,2,4‐triazin‐5‐one building blocks from commercially available material. By employing these building blocks, a practical protocol is described for the functionalization of the 5‐position of the triazine core with anilines orphenols. An optimized synthesis of 1,2,4‐triazines B and coupling with anilines and phenols to give C is described.