Synthesis and sedative-hypnotic activity of helicid derivatives containing a 1,4-dihydropyridine moiety

摘要

Reactions of natural helicid with a number of 1,3-dicarbonyl compounds or β-ketoester in the presence of ammonium acetate or 1-naphthylamine gave a series of helicid derivatives containing a 1,4-dihydropyridine fragment (2a-2h). Eight novel helicid derivatives were structurally confirmed by IR, 1H NMR, ~(13)C NMR, and HR-MS spectroscopy and evaluated for their sedative-hypnotic activities on mice. The results demonstrated that two compounds had higher sedative-hypnotic activity compared with helicid.