A mild and general protocol for the Pd(0)-catalyzed heteroannulation of o-bromoanilines and alkynes is described. Application of a Pd(0)/P((t)Bu)3 catalyst system enables the efficient coupling of o-bromoanilines at 60 °C, mitigating deleterious side reactions and enabling access to a broad range of useful unnatural tryptophans. The utility of this new protocol is demonstrated in the highly convergent total synthesis of the bisindole natural product (-)-aspergilazine A.
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| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC5505074 | PMC |
| http://dx.doi.org/10.1021/acs.orglett.6b02477 | DOI Listing |
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