Synthesis of C-11 methyl-substituted benzocycloheptapyridine inhibitors of farnesyl protein transferase |
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Authors: | Njoroge F G Vibulbhan B Wong J K White S K Wong S C Carruthers N I Kaminski J J Doll R J Girijavallabhan V Ganguly A K |
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Institution: | Schering-Plough Research Institute, Department of Chemistry, Kenilworth, New Jersey 07033, USA. |
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Abstract: | formula: see text] Synthesis of C-11 methyl-substituted benzocycloheptylpyridine tricyclic compounds has been achieved via two different methods. Methylation of C-11 has been effected by treatment of amine 4 with BuLi followed by Mel quenching. In a similar procedure, introduction of a C-11 substituent with concomitant rearrangement of the exocyclic double bond has been carried out. Potent farnesyl protein transferase inhibitors have been synthesized using the above methodologies. |
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