CAS: 39856-57-0; 2,6-Dibromopyridin-3-Amine

相似化合物

55304-80-8 39856-58-1 13534-97-9

上下游产品

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3-氨基吡啶置于n-溴代丁二酰亚胺(Nbs)体系中,用 四氯化碳 用作溶剂,化学反应 2.0H,以46%的收率获得2,6-二溴-3-氨基吡啶
参考文献:噻唑基肽抗生素ge2270 A的简明全合成.
标题:噻唑基肽抗生素ge2270 A的简明全合成.
摘要:由n-叔丁氧羰基保护的缬氨酸以最长的20步线性序列合成了有效的抗生素噻唑基肽ge2270 A,总产率为4.8%.关键策略是通过从2,6-二溴-3-碘吡啶开始的连续交叉偶联反应组装2,3,6-三取代吡啶核.通过3-锌的2,6-二溴吡啶的negishi交叉偶联将完整的southern片段安装在三噻唑的2-碘噻唑末端(87%).在通过另一个negishi交叉偶联金属化成锌试剂后,以截短的2-溴噻唑-4-羧酸叔丁酯形式引入代表分子北部的c-6处的取代基.整个序列的决定性步骤是将大环化成29元大环内酰胺,这是通过发生在吡啶核的c-2处的分子内stille交叉偶联进行的,以75%的收率提供所需的产物.通过在代表ge2270 A东部的复杂二噻唑片段与3,6-二取代的2-溴吡啶之间的酰胺键形成(87%)获得所需的锡烷.最终步骤包括将丝氨酸-脯氨酸酰胺二肽附着到分子的北部(65%),形成恶唑啉环和甲硅烷基醚脱保护(总体占55%).
Doi:10.1002/chem.200701823

专利信息

专利号:US-2022356182-A1
优先权日:2009-03-27
标题 :Inhibitors of hepatitis c virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-11053243-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOIL RICHARD; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

专利号:US-9090661-B2
优先权日:2009-03-27
标 题:Inhibitors of hepatitis C virus replication
发明人：COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.