19407-66-0Relevant academic research and scientific papers
Conversion of 2-thioxo-2,3-dihydroquinazolin-4(1H)-ones to N(3)-unsubstituted 2-(het)arylquinazolin-4(3H)-ones by copper-mediated Pd-catalysed cross-coupling reactions
Kri??iūnien?, Vilija,Matulevi?iūt?, Gita,Paliulis, Osvaldas,Rollin, Patrick,?a?kus, Algirdas
, p. 150 - 163 (2017/03/11)
With the purpose of searching for new heterocyclic building blocks, a new method to access N(3)-unsubstituted 2-(het)arylquinazolin-4(3H)-ones from 2-thioxo-2,3-dihydroquinazolin-4(1H)-one derivatives was developed. The synthetic protocol was based on the copper-mediated palladium-catalysed cross-coupling reactions of 2-thioxo-2,3-dihydroquinazolin-4(1H)-ones with (het)arylstannanes or their S-benzylated derivatives with (het)arylboronic acids, using CuBr·Me2S and CuMeSal as promoters, respectively. A similar transformation was applied for the preparation of 2-aryl[1]benzothieno[3,2-d]pyrimidin-4(3H)-ones.
Computer-aided design, synthesis and validation of 2-phenylquinazolinone fragments as CDK9 inhibitors with anti-HIV-1 tat-mediated transcription activity
Sancineto, Luca,Iraci, Nunzio,Massari, Serena,Attanasio, Vanessa,Corazza, Gianmarco,Barreca, Maria Letizia,Sabatini, Stefano,Manfroni, Giuseppe,Avanzi, Nilla Roberta,Cecchetti, Violetta,Pannecouque, Christophe,Marcello, Alessandro,Tabarrini, Oriana
, p. 1941 - 1953 (2014/01/06)
The activity of the cyclin-dependent kinase 9 (CDK9) is critical for HIV-1 Tat-mediated transcription and represents a promising target for antiviral therapy. Here we present computational studies that, along with preliminary synthetic efforts, allowed us
