Strategies to Macrocycles: Microwave approach

Totally Microwave

After coming across the phase separation strategy for preparing medium to large macrocycles with  a 1,3-diyne moiety, I thought about the holes in my background in this area — which is a bit strange considering I started my career at Abbott and with all the Erythromycin or macrolide chemistry performed there in general one would think I would have been up on it…alas, about as much as not finding Clarithromycin internally (not really a parting shot, but if the resident experts miss a billion dollar drug how am I expected to keep up — knowing the stories it is easy to miss). 😉

Usually the intro for this topic starts with clinically relevant and natural macrocyclic antibiotics — lots of them, but there is so much more from branching polycyclic peptides to the antifungal and antiparastics adding to the structural diversity. I certainly remember when the epothilone synthetic strategies came…

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