title: Synthesis of C-11 methyl-substituted benzocycloheptapyridine inhibitors of farnesyl protein transferase.
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.
authors.affiliation: Schering-Plough Research Institute, Department of Chemistry, Kenilworth, New Jersey 07033, USA.
authors.forename: F G
authors.initials: FG
authors.lastname: Njoroge
authors.forename: B
authors.initials: B
authors.lastname: Vibulbhan
authors.forename: J K
authors.initials: JK
authors.lastname: Wong
authors.forename: S K
authors.initials: SK
authors.lastname: White
authors.forename: S C
authors.initials: SC
authors.lastname: Wong
authors.forename: N I
authors.initials: NI
authors.lastname: Carruthers
authors.forename: J J
authors.initials: JJ
authors.lastname: Kaminski
authors.forename: R J
authors.initials: RJ
authors.lastname: Doll
authors.forename: V
authors.initials: V
authors.lastname: Girijavallabhan
authors.forename: A K
authors.initials: AK
authors.lastname: Ganguly
mesh_terms: D019883:Alkyl and Aryl Transferases / Q000037:antagonists & inhibitors*; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology
chemical_list: D004791:Enzyme Inhibitors; D011725:Pyridines; C409082:benzocycloheptapyridine; D019883:Alkyl and Aryl Transferases; C064911:p21(ras) farnesyl-protein transferase