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C2-dissymmetric PyOX-ligands have been applied to the asymmetric Henry reaction. This widely applicable reaction is easy to perform, requires no inert atmospheres or dry solvents, and gives good selectivities. By adjusting ligand side-chains, a significant impact on selectivities was observed.

A novel supported amino alcohol linker was synthesized and utilized for attachment of picolinic acid derivatives onto different supports. When the resin bound molecule was further activated, the PyOX-moiety could be constructed reliably in enantiopure form. Furthermore, an efficient Pd-catalyzed modification of a picolinic acid derivative is presented.

A short and convenient synthesis of a carboxy functionalized PyOX-core is presented. The carboxy functionality offers a wide variety of possibilities for further modification. In this paper, the core is functionalized with a mercapto tail.