Publications [#233221] of Andrew T. McPhail
Journal Articles
- Afonso, A; Kelly, J; Puar, MS; McCombie, S; McPhail, AT, "Synthesis of a C11 spiropiperidino derivative of 8-chloro-6,11- dihydro 5H-benzo[5,6]cyclohepta[1,2-b]pyridine", Tetrahedron LettersOctober,, 1998, 39(42), 7661-7664, Elsevier BV [Gateway.cgi], [doi].
(last updated on 2026/01/21)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.