Calum Macleod, B. Martínez-Teipel, W. Barker
2006
Citations
0
Influential Citations
25
Citations
Journal
ACS Combinatorial Science
Abstract
The microwave-assisted solid-phase synthesis of piperazines, 3,9-diazaspiro[5.5]undecanes and 2,9-diazaspiro[5.5]undecanes is reported. The synthesis relies on the direct annulation of primary amines with resin-bound bismesylates 12, 17, and 22. Critical to the success of this chemistry was the development of α-methyl benzyl carbamate resin linker. This resin permits the cleavage of the heterocycles under mildly acidic conditions, free of contaminating linker-derived N-alkylated byproducts.