Derivatives Of Menthol And Eugenol Derivatives And Natural Product Combretastatin A-4 Synthesis

It is described that the advances of research of the nonsteroidal anti-inflammatory drugs in this paper. 17 menthol derivatives and 14 eugenol derivatives have been designed and synthesized in which 20 are novel. All of their structures have been confirmed by ~1H-NMR and MS. The pharmacological tests showed that most derivatives synthesized exhibited the anti-inflammatory activites. The anti-inflammatory activity of WQ-1, WQ-2, WQ-5, WQ-10, WQ-11, YQ-2, YQ-12 and YQ-14 is good.In this paper, natural product Combretastatin A-4(CA-4) were investigated and synthesized, literature reported that most syntheses of CA-4 utilize Wittig reaction, and the majority of these products is trans isomer. However, the cis configuration of CA4 is the most important factor for inhibition of cancer cell growth. We utilized the Perkin condensation according to the literature, and the configuration of CA-4 is Cis. CA-4 was synthesized in 41.2% overall yield from the starting material gallic acid via methylation, esterification, deoxidation, chlorination, cyanidation, hydrolization, Perking condensation, deacetylating, decarboxylization etc. For decarboxylization we utilized microwavation which shorten reaction time and reduce reaction temperature.