SUN-N5030

Chemical Name: 1-Phenoxy-3-[4-(4-phenoxyphenyl)piperidin-1-yl]-2-propanol hydrochloride
CAS No. 254432-70-7, 254432-72-9 ((R)-isomer), 254432-73-0 ((S)-isomer)
项目整合开发状态: Preclinical
项目研究机构: Daiichi Suntory Pharma (Originator)
合成路线:Addition of the Grignard reagent prepared from 4-bromodiphenyl ether (I) to N-Boc-4-piperidone (II) gave the 4-hydroxy-4-arylpiperidine (III).Deprotection of the Boc group of (III) with concomitant dehydration of the tertiary alcohol by means of trifluoroacetic acid afforded the tetrahydropyridine (IV),which was further hydrogenated to piperidine (V) using Pd/C as the catalyst.Condensation of pieridine (V) with phenyl glycidyl ether (VI) in refluxing isopropanol yielded the desired amino alcohol,which was finally isolated as the corresponding hydrochloride salt.