Abstract
An effective synthesis which provides facile access to highly rigid tetraazamacrocycles possessing labile functional groups is reported. Essential to the approach is bis-bispidinone, a versatile substrate which can be prepared from an unusually stable bispidine diethyl ketal building block and requires a non-aqueous isolation process. Further functionalization of the substrate allows direct and concurrent incorporation of functionalities onto the bis-bispidine tetraazamacrocyclic framework, in particular those that are labile during the macrocycle formation.
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