Elsevier

Tetrahedron Letters

Volume 51, Issue 52, 29 December 2010, Pages 6852-6855
Tetrahedron Letters

Total synthesis of LL-Z1640-2 utilizing a late-stage intramolecular Nozaki–Hiyama–Kishi reaction

https://doi.org/10.1016/j.tetlet.2010.10.092Get rights and content

Abstract

A total synthesis of LL-Z1640-2 (2), a potent and selective kinase inhibitor, has been completed. The key step of the convergent synthesis utilized a late-stage intramolecular Nozaki–Hiyama–Kishi (NHK) reaction to close the macrocycle at the C6′–C7′ bond.

Graphical abstract

A total synthesis of LL-Z1640-2 (2), a potent and selective kinase inhibitor, has been completed. The key step of the convergent synthesis utilized a late-stage intramolecular Nozaki–Hiyama–Kishi (NHK) reaction to close the macrocycle at the C6′–C7′ bond.

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Acknowledgment

The authors thank William Leister for his assistance with normal and reverse phase purification techniques. This research was supported by the Molecular Libraries Initiative of the National Institutes of Health Roadmap for Medical Research, the Intramural Research Program of the National Human Genome Research Institute, and the National Institutes of Health.

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