CAS: 40925-68-6; 2-Amino-4-Bromophenol

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4-溴-2-硝基苯酚置于盐酸,Tin(II) Chloride Dihdyrate体系中,用 甲醇 作为反应溶剂,以94%的收率获得产物2-氨基-4-溴苯酚
参考文献:(+/-)-反式-2-苯基-2,3-二氢苯并呋喃类杀菌剂:合成,体外评估和sar分析.
标题:(+/-)-反式-2-苯基-2,3-二氢苯并呋喃类杀菌剂:合成,体外评估和sar分析.
摘要:利什曼病是由利什曼原虫属的寄生虫引起的一种被忽视的热带病,在世界范围内造成了严重的疾病负担,对数百万人的生命构成了威胁,因此是主要的公共卫生问题.需要更有效且无毒的新疗法,特别是对于内脏利什曼病(一种最严重的疾病).在二氢苯并呋喃以前具有抗霉菌活性的背景下,我们在此介绍一组70种反式-2-苯基-2,3-二氢苯并呋喃的合成及其对利什曼原虫donovani的体外活性的评估,并讨论结构-活动关系.化合物8M-O和8R表现出最高的效价(ic 50 <2μmol/ L)和抗真菌活性相对于对哺乳动物细胞的细胞毒性的有趣的选择性(si> 4.6).尽管如此,从体外代谢测定中观测到的最有效化合物(8M)的高清除率可以推断出结构优化是进一步的要求.另一方面,手性分离8M并随后对其对映异构体进行生物学评估表明,手性对活性和细胞毒性没有影响.通过简单的评分函数估算药物相似性对计算机模拟adme的性质和配体效率
DOI:10.1016/j.Ejmech.2020.112493

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:WO-2023072966-A1
优先权日:2021-10-26
标题:Imidazolone derivatives as inhibitors of protein kinases in particular dyrk1a, clk1 and/or clk4
发明人：DEAU EMMANUEL; GEORGE PASCAL; MEIJER LAURENT; MIEGE FRÉDÉRIC
权利人:PERHA PHARMACEUTICALS
摘要:The present invention relates to a compound of formula (I) wherein R 1 represents a (C 4 -C 6) alkyl group, a (C 3 -C 8) cycloalkyl group, a bridged (C 6 -C 10 )cycloalkyl group, a fused phenyl group, a substituted phenyl group, a R'-L- group, wherein L is either a single bond or a (C 1 -C 3 )alkanediyl group, and R' represents, a (C 3 -C 8 )heterocycloalkyl group, or a (C 3 -C 8 )heteroaryl group, or a R''-L- group wherein L is a (C 1 -C 3 )alkanediyl group, and R'' is an optionally substituted phenyl group; R 2 is selected from the group consisting of a hydrogen atom and a (C 1 -C 3 )alkyl group; R 5 represents a hydrogen atom, a (C 1 -C 4 )alkyl group or a (C 3 -C 6 )cycloalkyl group or any of its pharmaceutically acceptable salt. The present invention further relates to a composition comprising a compound of formula (I) and a process for manufacturing said compound as well as its synthesis intermediates. It also relates to said compound for use as a medicament, in particular in the treatment and/or prevention of cognitive deficits and neuroinflammation associated with Down syndrome; Alzheimer's disease; dementia; tauopathies; Parkinson's disease; CDKL5 Deficiency Disorder; Phelan-McDermid syndrome; autism; type 1 and type 2 diabetes; abnormal folate and methionine metabolism; osteoarthritis and tendinopathy; Duchenne muscular dystrophy; cancers and leukemias; neuroinflammation, anemia, infections caused by unicellular parasites, viral infections and for regulating body temperature.

专利号:CN-111606910-A
优先权日:2020-06-30
标 题:A kind of synthesis process of antitumor drug Sapanisertib

专利号:CN-119241459-A
优先权日:2024-09-03
标题:Benzo (A) benzo (B) benzo (A oxazole/benzo Synthesis method of thiazole compound