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Synthesis of a C11spiropiperidino derivative of 8-chloro-6,11-dihydro 5H-benzo[5,6]cyclohepta[1,2-b]pyridine

Authors
Journal
Tetrahedron Letters
0040-4039
Publisher
Elsevier
Publication Date
Volume
39
Issue
42
Identifiers
DOI: 10.1016/s0040-4039(98)01714-6

Abstract

Abstract 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.

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