CAS: 136434-77-0; 1-Bromo-2-Fluoro-4-Iodobenzene

上下游产品

3-fluoro-4-bromophenylamine 2-fluro-4-iodoaniline 2-Fluoroaniline meta-fluoroaniline 1-bromo-2-fluoro-4-pent-1-ynylbenzene 3-bromo-2-fluoro-6-iodo-benzoic acid 3-(4-bromo-3-fluorophenyl)-5-(hydroxymethyl)oxazolidin-2-one

2-氟-4-碘苯胺置于氢溴酸,Sodium Nitrite,Copper(I) Bromide体系中,用 水 用作溶剂,以23 %的收率获得1-溴-2-氟-4-碘苯
参考文献:结构引导的新型泛金属-β-内酰胺酶抑制剂的发现,具有改善的革兰氏阴性细菌细胞渗透性
标题:结构引导的新型泛金属-β-内酰胺酶抑制剂的发现,具有改善的革兰氏阴性细菌细胞渗透性
摘要:使用 β-内酰胺 (Bl) 和 β-内酰胺酶抑制剂组合来克服 Bl 抗生素耐药性已通过临床批准的药品得到验证.然而,对于治疗由表达金属-β-内酰胺酶的革兰氏阴性(gn)细菌引起的感染,仍然存在未满足的医疗需求.之前,我们报道了我们发现此类三个主要家族的泛抑制剂的努力:Imp,Vim 和 Ndm.在此,我们描述了我们与亚胺培南和瑞巴坦结合改善 Gn 覆盖范围的工作.这是通过基于结构和属性的优化来解决 Gn 细胞渗透和外排挑战而实现的.一项重大发现表明,抑制 Vim 等位基因 Vim-1 和 Vim-2 对于广泛的 Gn 覆盖至关重要,尤其是针对产生 Vim 的铜绿假单胞菌.此外,还对选定化合物的药代动力学和非临床安全性进行了研究.此次药物发现活动的主要发现为进一步优化先导化合物以识别临床前候选药物奠定了基础.
Doi:10.1021/acs.Jmedchem.3C01614

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.

专利号:US-9708336-B2
优先权日:2014-01-22
标题 :Metallo-beta-lactamase inhibitors
发明人：MANDAL MIHIR; TANG HAIFENG; XIAO LI; SU JING; LI GUOQING; YANG SHU-WEI; PAN WEIDONG; TANG HAIQUN; DEJESUS REYNALDA; HICKS JACQUELINE; LOMBARDO MATTHEW; CHU HONG; HAGMANN WILLIAM; PASTERNAK ALEX; GU XIN; JIANG JINLONG; DONG SHUZHI; DING FA-XIANG; LONDON CLARE; BISWAS DIPSHIKHA; YOUNG KATHERINE; HUNTER DAVID N; ZHAO ZHIQIANG; YANG DEXI
权利人:MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula (I) that are metallo-β-lactamase inhibitors, the synthesis of such compounds, and the use of such compounds for use with β-lactam antibiotics for overcoming resistance.

专利号:CN-102372618-B
优先权日:2011-10-20
标题 :Practical Synthesis of 2-Halo-1-(4-Bromo-3-fluorophenyl)ethanone

专利号:CN-102372618-A
优先权日:2011-10-20
标题:Practical Synthesis of 2-Halo-1-(4-Bromo-3-fluorophenyl)ethanone