Asymmetric synthesis of (S)-(−)-N-acetylcolchinol via Ullmann biaryl coupling |
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| Authors: | Simon D. Broady John Leonard James C. Muir |
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| Affiliation: | a Process R&D, AstraZeneca plc, Silk Road Business Park, Macclesfield, Cheshire SK10 2NA, UK
b AstraZeneca Pharma, Z.I. Pompelle, BP 1050, 51689 Reims, Cedex 2, France |
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| Abstract: | A modified Ziegler Ullmann coupling process has been developed as the key step in an effective synthesis of (S)-(−)-N-acetylcolchinol, analogues of which are selective vascular targeting agents with potential importance in cancer chemotherapy. Asymmetric induction is achieved by enamide hydrogenation using FerroTANE catalysts. |
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