72398-89-1Relevant academic research and scientific papers
Method for synthesizing o-alkenyl phenol derivative through ring opening of benzofuran under catalysis of nickel
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Paragraph 0042; 0144-0150, (2021/07/14)
The invention belongs to the technical field of organic synthesis, and discloses a method for synthesizing an o-alkenyl phenol derivative through ring opening of benzofuran under catalysis of nickel. The method comprises the following step: in a protective atmosphere and with an organic solvent as a reaction medium, subjecting a benzofuran compound to reacting with a silicon-hydrogen compound under the action of a nickel catalyst and a ligand or the action of the nickel catalyst, the ligand and an additive to obtain a product containing a silicon protecting group, namely the o-alkenyl phenol derivative containing the silicon protecting group; or removing the silicon-containing protecting group to obtain the o-alkenyl phenol derivative, namely the o-alkenyl phenol derivative containing the phenolic hydroxyl group. According to the method, nickel is used as a catalyst, a phosphine compound or N-heterocyclic carbene is used as a ligand, and the method has the advantages of high yield, wide substrate applicability and the like. In addition, the benzofuran compound is used as a raw material in the reaction, so the method has the advantages of cheap and easily available raw materials, simplicity and convenience in operation, mild reaction conditions, good functional group position compatibility and the like, and has very high practicability.
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.
