Synthetic strategy, macrolide synthesis

In Section II, the synthetic strategies for macrolide synthesis are introduced and focus in particular on asymmetric synthesis of 1,3-diol, synthetic methodology for macrolactone, and glycosidation. In Section III, the total synthesis of selected macrolide antibiotics is introduced FK506 (tacrolimus 1), rapamycin (sirolimus 2), avermectins (3), altohyrtins (spongistatins 4), and epothilones (5) (Fig. 1). Several other synthesized macrolides are also illustrated. 

A number of new macrolide antibiotics with interesting bioactivity have been isolated, and the unique and complex structures have been determined. Toward the total synthesis of such attractive macrolide antibiotics, very efficient synthetic strategies and useful methodologies have been developed. Recent advances in macrolide synthesis based on newly developed strategies and methodologies are remarkable various complex macrolides having many chiral centers have been efficiently synthesized with excellent stereoselectivity. Recently, combinatorial... 

Although the absolute configuration has only been established for a few polyene macrolide antibiotics, the search for new, efficient, and selective strategies for the synthesis of their polyol structures is in full swing. A number of the synthetic procedures presented here will certainly be used in future syntheses of this class of natural products [19]. 

Ghosh, A.K., Mathivanan, P and Cappiello, J. (1997) Synthetic studies of antitumor macrolide laulimalide enantioselective synthesis of the Cj-C]4 segment by a catalytic hetero Dids-Alder strategy. Tetrahedron Lett., 38, 2427-2430. 

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