ABSTRACT
The recently developed transition metal-mediated olefin metathesis has been utilized in a number of solid-phase syntheses for the construction of rings of various sizes, including several examples of macrocycles that would be inaccessi-ble by other solid-phase synthetic methods (Fig. 7) [59-61]. The generality of the method has made olefin metathesis a useful tool for the synthesis of various macrocycles. The resulting cyclic scaffolds are preferred over their linear counterparts since they often bind more tightly to proteins, due in part to their reduced entropy of binding. Medicinal chemists also glean additional structural information from leads discovered from these compound libraries, since their mode of binding can be predicted with greater precision due to decreased conformational flexibility of the molecules.
