OPC-28326

Chemical Name: N-[2,6-Dimethyl-4-[4-[N-methyl-N-(2-phenylethyl)amino]piperidin-1-ylcarbonyl]phenyl]propionamide hydrochloride monohydrate
项目整合开发状态: Phase II
项目研究机构: Otsuka (Originator)
合成路线:Condensation of N-benzyl-4-piperidinone (I) with phenethylamine (II) produced the corresponding imine (III),which was subsequently reduced to amine (IV) using NaBH4.Schweiler-Clarke methylation of the secondary amine (IV) in the presence of formaldehyde and formic acid gave (V).The N-benzyl protecting group of (V) was then removed by catalytic hydrogenation,yielding piperidine (VI).This was finally coupled with 3,5-dimethyl-4-propionamidobenzoic acid (VII) by means of diethyl cyanophosphate to produce the target compound,which was isolated as the hydrochloride salt.