CAS: 697761-98-1; (S)-6-(3-Chloro-2-Fluorobenzyl)-1-(1-Hydroxy-3-Methylbutan-2-yl)-7-Methoxy-4-Oxo-1,4-Dihydroquinoline-3-Carboxylic Acid

上下游产品

6-(3-chloro-2-fluorobenzyl)-7-fluoro-1-((S)-1-hydroxymethyl-2-methylprop-1-yl)-4-oxo-1,4-dihydroquinoline-3-carboxylic acid sodium methylate 3-chloro-2-fluorobenzyl zinc bromide

1-(5-Iodo-2,4-Dimethoxyphenyl)Ethan-1-One置于盐酸,Bis-Triphenylphosphine-Palladium(II) Chloride,Sodium Hydride,Sodium Hydroxide体系中,用 四氢呋喃,甲醇,水,N,N-二甲基甲酰胺,甲苯 作为反应溶剂,化学反应 46.0H,反应生成 埃替拉韦
参考文献:Elvitegravir的改进合成
标题:Elvitegravir的改进合成
摘要:开发了一种新的hiv整合酶抑制剂elvitegravir(1)的活性药物成分的改进方法.它从市售的2,4-二甲氧基苯乙酮开始,将其选择性卤化至位置5.将5卤代苯乙酮与碳酸二烷基酯缩合,得到相应的苯甲酰乙酸酯.他们先用n,N-二甲基甲酰胺二甲基乙缩醛,再用(S)-缬氨醇处理,得到相应的中间体丙烯酸苯甲酰酯.通过用n,O处理可以实现芳香族亲核取代2-甲氧基,从而环化为所需的1,4-二氢喹啉-4-氧代衍生物.-双(三甲基甲硅烷基)-乙酰胺,它也作为三甲基甲硅烷基衍生物保护羟基.最后,Negishi与2-氟-3-氯苄基溴化锌的偶联以及随后的水解反应提供了elvitegravir(1).首选的变体是从2,4-二甲氧基苯乙酮开始的七步法,可提供29.3%的依维韦韦.
DOI:10.1002/jhet.2477

专利信息

专利号:US-2024400552-A1
优先权日:2016-11-11
标题 :Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS I; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by dysregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-11622968-B2
优先权日:2011-03-08
标 题:Heterocyclic modulators of lipid synthesis
发明人：BUCKLEY DOUGLAS; DUKE GREGORY; WAGMAN ALLAN S; EVANCHIK MARC; MCDOWELL ROBERT S
权利人:SAGIMET BIOSCIENCES INC
摘要:Compounds that are fatty acid synthesis modulators are provided. The compounds may be used to treat disorders characterized by disregulation of the fatty acid synthase function by modulating the function and/or the fatty acid synthase pathway. Methods are provided for treating such disorders including viral infections, such as hepatitis C infection, cancer and metabolic disorders, such as non-alcoholic steatohepatitis (NASH).

专利号:US-5935946-A
优先权日:1997-07-25
标 题 :Nucleotide analog composition and synthesis method
发明人：MUNGER JR JOHN D; ROHLOFF JOHN C; SCHULTZE LISA M
权利人:GILEAD SCIENCES INC
摘要:The invention provides a composition comprising bis(POC)PMPA and fumaric acid (1:1). The composition is useful as an intermediate for the preparation of antiviral compounds, or is useful for administration to patients for antiviral therapy or prophylaxis. The composition is particularly useful when administered orally. The invention also provides methods to make PMPA and intermediates in PMPA synthesis. Embodiments include lithium t-butoxide, 9-(2-hydroxypropyl) adenine and diethyl p-toluenesulfonylmethoxyphosphonate in an organic solvent such as DMF. The reaction results in diethyl PMPA preparations containing an improved by-product profile compared to diethyl PMPA made by prior methods.

专利号:EP-2906529-B1
优先权日:2012-10-12
标题:A new production method and new intermediates of synthesis of elvitegravir

专利号:EP-2906529-A1
优先权日:2012-10-12
标 题 :A new production method and new intermediates of synthesis of elvitegravir

专利号:EP-2906529-B9
优先权日:2012-10-12
标题:A new production method and new intermediates of synthesis of elvitegravir
发明人：RADL STANISLAV
权利人:ZENTIVA KS