877130-28-4Relevant articles and documents
Synthesis of filibuvir. Part III. Development of a process for the reductive coupling of an aldehyde and a β-keto-lactone
Ide, Nathan D.,Ragan, John. A.,Bellavance, Gabriel,Brenek, Steve J.,Cordi, Eric M.,Jensen, Grace O.,Jones, Kris N.,France, Danny La,Leeman, Kyle R.,Letendre, Leo J.,Place, David,Stanchina, Corey L.,Sluggett, Gregory W.,Strohmeyer, Holly,Blunt, Jon,Meldrum, Kevin,Taylor, Stuart,Byrne, Ciaran,Lynch, Denis,Mullane, Sandra,O'Sullivan, Maria M.,Whelan, Marcella
, p. 45 - 56 (2014/05/20)
Development of a reductive coupling of a β-keto-lactone and an aldehyde is described, in which the Hantzsch ester serves as an inexpensive and convenient reducing agent. Structural features in the β-keto-lactone rendered standard reductive coupling conditions ineffective, requiring development of a specific addition and temperature protocol. Identification of one of the reactants as Ames positive required a single-digit parts per million control strategy for this impurity in the final active pharmaceutical ingredient (API).
Synthetic route optimization of PF-00868554, an HCV polymerase inhibitor in clinical evaluation
Johnson, Sarah,Drowns, Matt,Tatlock, John,Linton, Angelica,Gonzalez, Javier,Hoffman, Robert,Jewell, Tanya,Patel, Leena,Blazel, Julie,Tang, Mingnam,Li, Hui
scheme or table, p. 796 - 800 (2010/06/13)
This paper describes the optimization efforts to establish an enabling synthesis to provide multigram quantity of PF-00868554, an HCV polymerase inhibitor currently in phase II clinical evaluations.
METHODS FOR THE PREPARATION OF HCV POLYMERASE INHIBITORS
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Page/Page column 65-66, (2008/06/13)
The present invention relates to methods and compounds useful in the preparation of compounds of the formula (I).