Journal of Organic Chemistry p. 4873 - 4892 (2019)
Update date:2022-08-04
Topics:
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.
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.
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