AHL-157

合成路线:Protected piperidone (I) is condensed with methoxybromobenzene (II) via Grignard reaction by means of Mg and catalytic iodine in refluxing THF,and the resulting alcohol is then dehydrated with refluxing HCl in dioxane to afford compound (III).Hydrogenation of tetrahydropyridine (III) over Pd/C in EtOH yields piperidine derivative (IV),which is then demethylated with aqueous HBr to provide phenol (V).Condensation of (V) with 4-fluorobenzoyl chloride (VI) by means of NaOH in iPrOH/MeOH/H2O furnishes N-benzoylpiperidine derivative (VII),which is converted into the desired product by reaction with ethyl 2-bromo-2-methylpropanoate (VIII) by means of K2CO3 followed by hydrolysis with NaOH in H2O/MeOH/dioxane.

参考文献标题:Preparation of new fibrates with piperidine ring and the pharmacological activity
文献作者:Komoto,T.; et al.
参考来源:20th Symp Med Chem (Dec 6 2000,Tokyo) 2000,Abst 2P-06


合成路线:Protected piperidone (I) is condensed with methoxybromobenzene (II) via Grignard reaction by means of Mg and catalytic iodine in refluxing THF,and the resulting alcohol is then dehydrated with refluxing HCl in dioxane to afford compound (III).Hydrogenation of tetrahydropyridine (III) over Pd/C in EtOH yields piperidine derivative (IV),which is then demethylated with aqueous HBr to provide phenol (V).Condensation of (V) with 4-fluorobenzoyl chloride (VI) by means of NaOH in iPrOH/MeOH/H2O furnishes N-benzoylpiperidine derivative (VII),which is converted into the desired product by reaction with ethyl 2-bromo-2-methylpropanoate (VIII) by means of K2CO3 followed by hydrolysis with NaOH in H2O/MeOH/dioxane.
参考文献标题:New strong fibrates with piperidine moiety
文献作者:Komoto,T.; Hirota,T.K.; Otsuka,M.; Kotake,J.; Hasegawa,S.; Koya,H.; Sato,S.; Sakamoto,T.
参考来源:Chem Pharm Bull 2000,48(12),1978


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