Abstract:A new synthetic protocol leading to vascular disrupting agent (Z)-3′-amino-3,4,4′,5-tetramethoxylstilbene (AVE-8063) was successfully devised. Starting from 4-methoxyphenylacetic acid, (E)-2-(3-bromo-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl) acrylic acid (Ⅲ) could readily be obtained through bromination and Perkin condensation. Amination of (Ⅲ) afforded (E)-2-(3-animo-4-methoxyphenyl)-3-(3,4,5-trimethoxyphenyl)acrylic acid (Ⅳ), which was subsequently decarboxylated in Cu/1,10-Phen/PEG-400 system under microwave conditions for 6 min to give the target product (Ⅴ) with 60.1% total yield. The structure of the product was verified by IR, MS and 1H NMR.