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Published on: March 29, 2018
Skeletal diversity via a branched pathway: efficient synthesis of 29 400 discrete, polycyclic compounds and their
Ohyun Kwon1, Seung Bum Park, Stuart L Schreiber
1Department of Chemistry and Chemical Biology, Howard Hughes Medical Institute, Harvard Institute of Chemistry and Cell Biology, Harvard University, 12 Oxford Street, Cambridge, Massachusetts 02138, USA.
Abstract:
We report the synthesis and arraying of 29 400 structurally diverse and complex polycyclic carbocycles using diversity-oriented synthesis (DOS) and the "one bead-one stock solution" technology platform. Skeletal diversity, a difficult challenge in DOS, was achieved with a branching reaction pathway using one or two Diels-Alder reactions. This pathway yields small molecules having 10 different skeletons.
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