72398-88-0Relevant academic research and scientific papers
Aryiolefins compound synthetic method
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Paragraph 0045; 0046; 0047; 0048, (2016/10/09)
The invention discloses an aryiolefins compound synthetic method and belongs to the field of organic chemistry synthesis. The aryiolefins compound synthetic method particularly includes dissolving an o-hydroxy (amino) aryl alkynes compound, a bis(pinacolato) borate compound, a transition metal (rhodium, iridium, palladium or platinum), alkali and a hydrogen source into an organic solvent at a nitrogen atmosphere prior to heating and stirring reaction, removing the organic solvent under reduced pressure after the reaction is terminated, and conducting column chromatography separation so as to obtain various o-hydroxy (amino) aryiolefins compounds. Compared with an existing method, the aryiolefins compound synthetic method has the advantages of simpler synthetic and reaction steps, mild reaction conditions, simplicity, convenience and feasibility in operation, cheap and easily available raw materials and capabilities of reaching more than 80% in product yield, inhibiting production of cyclization product benzofuran or indole derivatives and improving reaction efficiency and reactive atom economy, thereby being a novel approach to synthesis of the o-hydroxy (amino) aryiolefins compounds.
Syntheses and Platelet Aggregation Inhibitory and Antithrombotic Properties of ethyl>benzenes
Kikumoto, Ryoji,Hara, Hiroto,Ninomiya, Kunihiro,Osakabe, Masanori,Sugano, Mamoru,et al.
, p. 1818 - 1823 (2007/10/02)
A series of ethyl>benzene derivatives were synthesized and evaluated for their ability to inhibit collagen-induced platelet aggregation in vitro and to protect experimantal thrombosis in mice.The results showed that the compounds were in vitro inhibitors of collagen-induced platelet aggregation.Most of them were also effective in the mouse antithrombotic assay.The compounds were found to be potent antagonists to S2 serotonergic receptor, and good correlation (r = 0.85) between their S2 serotonergic receptor antagonism and their potency as platelet antiaggregatory drugs was observed.Among the compounds studied, monophenoxy>methyl>ethyl>succinate hydrochloride (12b, MCI-9042) was selected for further pharmacological and toxicological evaluation.
