304650-02-0Relevant articles and documents
Preparation method of dasabuvir key intermediate
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Paragraph 0015; 0020-0045, (2020/08/27)
The invention discloses a preparation method of a dasabuvir key intermediate. The preparation method comprises the following steps: carrying out substitution reaction on a compound A, namely 2-bromobenzonitrile, and a compound B, namely 2-picolinamide, so
Discovery and Development of Metal-Catalyzed Coupling Reactions in the Synthesis of Dasabuvir, an HCV-Polymerase Inhibitor
Barnes, David M.,Shekhar, Shashank,Dunn, Travis B.,Barkalow, Jufang H.,Chan, Vincent S.,Franczyk, Thaddeus S.,Haight, Anthony R.,Hengeveld, John E.,Kolaczkowski, Lawrence,Kotecki, Brian J.,Liang, Guangxin,Marek, James C.,McLaughlin, Maureen A.,Montavon, Donna K.,Napier, James J.
, p. 4873 - 4892 (2019/02/05)
Dasabuvir (1) is an HCV polymerase inhibitor which has been developed as a part of a three-component direct-acting antiviral combination therapy. During the course of the development of the synthetic route, two novel coupling reactions were developed. First, the copper-catalyzed coupling of uracil with aryl iodides, employing picolinamide 16 as the ligand, was discovered. Later, the palladium-catalyzed sulfonamidation of aryl nonaflate 33 was developed, promoted by electron-rich palladium complexes, including the novel phosphine ligand, VincePhos (50). This made possible a convergent, highly efficient synthesis of dasabuvir that significantly reduced the mutagenic impurity burden of the process.
Palladium-catalyzed carbonylative synthesis of N-(2-cyanoaryl)benzamides and sequential synthesis of quinazolinones
Wu, Xiao-Feng,Oschatz, Stefan,Sharif, Muhammad,Beller, Matthias,Langer, Peter
supporting information, p. 23 - 29 (2014/01/06)
A convenient procedure for the synthesis of N-(2-cyanoaryl)benzamides has been developed. Using aryl bromides and 2-aminobenzonitriles as the substrates, Mo(CO)6 as the CO source, the desired amides were produced in good yields. Quinazolinones
