N-苄氧羰酰基-2-甲基丙氨酸 在 盐酸羟胺,氯甲酸乙酯,三乙胺,三氟乙酸酐,Potassium Hydroxide体系中,用 四氢呋喃,二氯甲烷,氯仿,水,异丙醇作为反应溶剂,反应 52.0H,获得 Methyl 2-(2(((Benzyloxy)Carbonyl)Amino)Propan-2-yl)-5,6-Dihydroxy-1,6-Dihydropyrimidine-4-Carboxylate
参考文献:Hydroxyl May Not Be Indispensable For Raltegravir: Design,Synthesis And Sar Studies Of Raltegravir Derivatives As Hiv-1 Inhibitors
标题:Hydroxyl May Not Be Indispensable For Raltegravir: Design,Synthesis And Sar Studies Of Raltegravir Derivatives As Hiv-1 Inhibitors
摘要:A Series Of Raltegravir Derivatives 20-42 Were Prepared And Systematically Evaluated For Their Anti-Hiv Activity. The Bioassay Results Showed That Most Of The Compounds Possess Good To Excellent Anti-Hiv Activity. Especially,Compounds 25 And 35 With Subpicomole Ic50 Values Seemed To Be The Most Potent Anti-Hiv Agents Among All Of The Reported Synthesized Compounds. These Compounds May Therefore Be Considered As New Potent Anti-Hiv Agents. The 5-Hydroxyl Modification Of Raltegravir Derivatives Significantly Increased The Anti-Hiv Activity,Which Indicates That The Hydroxyl May Not Be Indispensable For Raltegravir. The Introducing Of Acyl At 5-Position Of Raltegravir Derivatives Is Favorable For Antiviral Activity. In Addition,A High-Throughput Cell-Based Assay Method With Pseudotyped Virus Stoks Was Developed And Used To Identify Hiv Inhibitors. (C) 2012 Elsevier Masson Sas. All Rights Reserved.
Doi:10.1016/J.Ejmech.2012.02.015