-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	44407
标题:	Phenylsulphonyl derivs. as 5-HT receptor ligands
作者:	Macleod, A.M.; Blurton, P.; Fletcher, S.R.; Van Niel, M.B.; Burkamp, F.; Cheng, S.K.-F. (Merck Sharp & Dohme Ltd.)
来源:	EP 1147083; WO 0043362

合成路线图解说明: The (phenylsulfanyl)piperidine (III) was obtained by condensation of N-Boc-4-piperidinol (I) with diphenyl disulfide (II) in the presence of tributylphosphine. Subsequent oxidation of sulfide (III) to the corresponding sulfone (IV) was achieved using oxone?on wet alumina. Deprotection of the N-Boc-piperidine (IV) with HCl afforded piperidine (V), which was finally alkylated with 2-bromo-4'-fluoroacetophenone (VI) to furnish the title N-phenacyl piperidine.

参考文献No.	647816
标题:	4-(Phenylsulfonyl)piperidines: Novel, selective, and biovailable 5-HT2A receptor antagonists
作者:	Fletcher, S.R.; Burkamp, F.; Blurton, P.; Cheng, S.K.; Clarkson, R.; O'Connor, D.; Spinks, D.; Tudge, M.; van Niel, M.B.; Patel, S.; Chapman, K.; Marwood, R.; Shepheard, S.; Bentley, G.; Cook, G.P.; Bristow, L.J.; Castro, J.L.; Hutson, P.H.; et al.
来源:	J Med Chem 2002,45(2),492

合成路线图解说明: The (phenylsulfanyl)piperidine (III) was obtained by condensation of N-Boc-4-piperidinol (I) with diphenyl disulfide (II) in the presence of tributylphosphine. Subsequent oxidation of sulfide (III) to the corresponding sulfone (IV) was achieved using oxone?on wet alumina. Deprotection of the N-Boc-piperidine (IV) with HCl afforded piperidine (V), which was finally alkylated with 2-bromo-4'-fluoroacetophenone (VI) to furnish the title N-phenacyl piperidine.