期刊
SYNTHESIS-STUTTGART
卷 -, 期 2, 页码 217-222出版社
GEORG THIEME VERLAG KG
DOI: 10.1055/s-0030-1258358
关键词
combretastatin A-4; combretastatin A-4 phosphate; renewable sources; green synthesis; Perkin reaction
资金
- Science and Technology Program of Guangdong Province
- Strategic Cooperation Program between Guangdong Province
- Chinese Academy of Sciences
- National Key Technology R & D Program, P. R. China [2003B31603, 2006B35604002, 2009B091300125, 2007BAD82B02]
A practical and green protocol for the synthesis of vascular disrupting agent combretastatin A-4 (CA4) and its water soluble prodrug CA4P is described. Starting from the biomass-based compound anethole, which is abundantly and sustainably available from Chinese star anise (Illicium verum Hook. f.), the key intermediate 3-hydroxy-4-methoxyphenylacetic acid can be obtained within five steps. Perkin condensation between this acid and another naturally derived compound 3,4,5-trimethoxybenzaldehyde, followed by decarboxylation gives combretastatin A-4 in good overall yield. The phosphate produrg CA4P can be prepared under simple and mild conditions in a sequential one-pot two-step reaction.
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