📜1-Cbz-4-哌啶酮置于palladium 10% On Activated Carbon,氢气,对甲苯磺酸体系中,用 甲醇,甲苯 用作溶剂,135.0~140.0 °C,101.33 Kpa 条件下,反应生成1,5-二叠氮-9-壬烯[5.5]十一烷
参考文献:Design And Synthesis Of Spirocyclic Compounds As Hcv Replication Inhibitors By Targeting Viral Ns4B Protein
标题:Design And Synthesis Of Spirocyclic Compounds As Hcv Replication Inhibitors By Targeting Viral Ns4B Protein
摘要:Two Novel Series Of Spirocyclic Piperidine Analogs Appended To A Pyrazolo[1,5-Alpha] Pyridine Core Were Designed,Synthesized And Evaluated For Their Anti-Hcv Activity. A Series Of Piperidine Ketals Afforded Dispiro 6P Which Showed Excellent In Vitro Anti-Hcv Activities (Ec50 Of 1.5 Nm And 1.2 Nm Against Genotype 1A And 1B Replicons,Respectively). A Series Of Piperidine Oxazolidinones Afforded 27C Which Showed Ec50'S Of 10.9 Nm And 6.1 Nm Against 1A And 1B Replicons,Respectively. Both Compounds 6P And 27C Bound Directly To Non-Structural Ns4B Protein In Vitro (Ic50'S = 10.2 And 30.4 Nm,Respectively) And Exhibited Reduced Potency In Replicons Containing Resistance Mutations Encoding Changes In The Ns4B Protein. (C) 2014 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Bmcl.2014.03.080