PD-174494, Co-101244

1-[2-(4-羟基苯氧基)乙基]-4-(4-甲基苄基)-4-哌啶醇盐酸盐(1:1) Chemical Name: 1-[2-(4-Hydroxyphenoxy)ethyl]-4-(4-methylbenzyl)piperidin-4-ol hydrochloride
CAS No. 193356-17-1, 193359-26-1 (free base), 222421-41-2 (hemifumarate)
项目整合开发状态: Preclinical
项目研究机构: CoCensys (Originator), Pfizer (Originator)
合成路线:The Grignard reagent (II),prepared form 4-methylbenzyl chloride (I),was condensed to N-benzyl-4-piperidone (III) in cold THF to provide the 4-hydroxy-4-benzylpiperidine (IV).Catalytic hydrogenolysis of the N-benzyl group of (IV) over Pd/C gave piperidine (V),which was then alkylated with 2-(4-benzyloxyphenoxy)ethyl bromide (VI) in refluxing acetonitrile to afford (VII).The O-benzyl group of (VII) was finally cleaved by hydrogenolysis in the presence of Pd(OH)2 to furnish the target compound.