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

Organic Process Research and Development

Volumn 8, Issue 4, 2004, Pages 643-650

  Andresen, Brian M ^a   Couturier, Michel ^a   Cronin, Brian ^a   D'Occhio, Michael ^a   Ewing, Marcus D ^a   Guinn, Mark ^a   Hawkins, Joel M ^a   Jasys, V John ^a   LaGreca, Susan D ^a   Lyssikatos, Joseph P ^a   Moraski, Garrett ^a   Ng, Karl ^a   Raggon, Jeffrey W ^a   Stewart, A Morgan ^a   Tickner, Derek L ^a   Tucker, John L ^a   Urban, Frank J ^a   Vazquez, Enrique ^a   Wei, Lulin ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

PROTEIN FARNESYLTRANSFERASE INHIBITOR;

ARTICLE; DRUG SYNTHESIS; GRIGNARD REACTION;

EID: 4243157453     PISSN: 10836160     EISSN: None     Source Type: Journal    
DOI: 10.1021/op049935g     Document Type: Article

References (7)

1. Kohl, N. E.; Mosser, S. D.; deSolms, S. J.; Giuliani, E. A.; Pompliano, D. L.; Graham, S. L.; Smith, R. L.; Scolnick, E. M.; Oliff, A.; Gibbs, J. B. Science 1993, 260, 1934.
2. Lyssikatos, J. P.; LaGreca, S. D. U.S. Patent 6,150,377, 2000.
3. Blackwell, J.; Hickinbottom, W. J. J. Chem Soc. 1963, 366.
4. Tang, C. C.; Davalian, D.; Huang, P.; Breslow, R. J. Am. Chem. Soc. 1978, 100, 3918.
5. El Boria, M.; Moustafa, A. H.; Anwar, M.; Ghatts, A. G. Croatia Chem. Acta 1981, 54, 211.
6. Turner, R. M.; Lindell, S. D.; Ley, S. V. J. Org. Chem. 1991, 56, 5739.
7. Purification through the hydrate tartaric acid salt form brings finished goods within specifications but results in a 30% attrition of the drug substance.