An Efficient Synthetic Strategy for Obtaining 4-Methoxy Carbon Isotope Labeled Combretastatin A-4 Phosphate and Other Z-Combretastatins

作者：Pettit George R^*; Minardi Mathew D; Hogan Fiona; Price Pat M

来源：Journal of Natural Products, 2010, 73(3): 399-403.

DOI：10.1021/np9004486

Human cancer and other clinical trials under development employing combretastatin A-4 phosphate (1b, CA4P) should benefit front the availability of a [(14)C]-labeled derivative for positron emission tomography (PET). In order to obtain it suitable precursor for addition of [(14)C]methyl group at the penultimate step several new synthetic pathways to CA4P Were evaluated. Geometrical isomerization (Z to E) proved to be a challenge, but it was overcome by development of a new CA4P synthesis suitable for 4-methoxy isotope labeling.

• 出版日期2010-3