Development of a Practical Synthesis of Toll-like Receptor Agonist PF-4171455: 4-Amino-1-benzyl-6-trifluoromethyl-1,3-dihydroimidazo [4,5-c] pyridin-2-one

• Published in: Organic process research & development Vol. 15; no. 4; pp. 788 - 796
• Main Authors: Adam, Fiona M, Bish, Gerwyn, Calo, Frederick, Carr, Christopher L, Castro, Nieves, Hay, Duncan, Hodgson, Paul B, Jones, Peter, Knight, Craig J, Paradowski, Michael, Parsons, Gemma C, Proctor, Katie J. W, Pryde, David C, Rota, Filippo, Smith, Mya C, Smith, Nicholas, Tran, Thien-Duc, Hitchin, James, Dixon, Rachel
• Format: Journal Article
• Language: English
• Published: American Chemical Society 15.07.2011

The development and implementation of a scalable process for the manufacture of the Toll-like receptor (TLR7) agonist PF-4171455 (1) is described. Initial routes used to synthesise 1 in milligram quantities were unsuitable for large-scale synthesis to provide bulk material. As part of the transfer b...