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

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

Tetrahedron letters (2011-04-26)
Christopher A Leclair, Matthew B Boxer, Craig J Thomas, David J Maloney
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.

MATERIALS
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Product Description

Sigma-Aldrich
Vinylboronic acid pinacol ester, contains phenothiazine as stabilizer, 95%