Synthesis of a C11 spiropiperidino derivative of 8-chloro-6,11- dihydro 5H-benzo[5,6]cyclohepta[1,2-b]pyridine
Journal Article
A method using N-tosyl aziridine for the synthesis of a spiropiperidine 2 (R=H) is described. Cleavage of the N-tosyl group of the intermediate 8 to form the spiropiperidinone 9 was found to proceed in high yield with conc. sulfuric acid. Acylated derivatives of 2 were required for a structure- activity study aimed at defining the spatial requirements of the N-acyl residue in the lead Farnesyl-Protein-Transferase inhibitor 1.
Full Text
Duke Authors
Cited Authors
- Afonso, A; Kelly, J; Puar, MS; McCombie, S; McPhail, AT
Published Date
- October 15, 1998
Published In
Volume / Issue
- 39 / 42
Start / End Page
- 7661 - 7664
International Standard Serial Number (ISSN)
- 0040-4039
Digital Object Identifier (DOI)
- 10.1016/S0040-4039(98)01714-6
Citation Source
- Scopus