In order to continuously supply CIJ-3-2F for further investigation on pharmacological mechanism, the author expects for a new synthetic strategy to elevate the yield and lower the damage to environment and human health.
The original synthetic method of CIJ-3-2F utilized toxic DMF as solvent to perform alkylation, and toxic diphenyl ether as heat transfer medium to achieve cyclization. The post-treatment process of DMF and Diphenyl ether is more difficult and harmful to human health. According to the recently-advocated green chemistry, the author tries to use ethanol, which produces less effect to environment, as solvent to perform alkylation and polyphosphoric acid to undergo Polyphosphoric acid catalyzed cyclization
CIJ-3-2F was proved to possess obvious antiarrhythmic activity. The antiarrhythmic effect of CIJ-3-2F was achieved via vasodilation. While acting on smooth muscle cells, CIJ-3-2F caused vasodilation by inducing the release of NO and activating guanylate cyclase. Besides, The CIJ-3-2F inhibited the influx of Ca2+ as well as IP3-induced intracellular Ca2+ release，stimulated the opening of voltage-dependent K+ channel, and thus produced the vasodilative effect.
