Streamlined processes for the synthesis of a farnesyl transferase inhibitor drug candidate

…, M Couturier, B Cronin, M D'Occhio…

Index: Andresen, Brian M.; Couturier, Michel; Cronin, Brian; D'Occhio, Michael; Ewing, Marcus D.; Guinn, Mark; Hawkins, Joel M.; Jasys, V. John; LaGreca, Susan D.; Lyssikatos, Joseph P.; Moraski, Garrett; Ng, Karl; Raggon, Jeffrey W.; Stewart, A. Morgan; Tickner, Derek L.; Tucker, John L.; Urban, Frank J.; Vazquez, Enrique; Wei, Lulin Organic Process Research and Development, 2004 , vol. 8, # 4 p. 643 - 650

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Citation Number: 31

Abstract

As part of a fast-paced oncology program, quinolinone 1 was discovered and developed as a potent inhibitor of farnesyl transferase for the treatment of cancer. The initial synthesis, which suffered from a lengthy linear sequence and a late-stage chromatographic resolution, was deemed not amenable to large-scale production. While investigating alternate routes to address these issues, the original synthesis was successively improved and streamlined. ...