CAS: 387-44-0; 7-Fluoroindole

上下游产品

7-fluoro-1H-indole-2-carboxylic acid vinyl magnesium bromide ortho-nitrofluorobenzene 4-bromo-7-fluoro-1H-indole 3-(7-fluoro-1H-indol-3-yl)-2,5-dichloro[1,4]benzoquinone H-indol-3-yl)-ethanone2,2,2-trifluoro-1-(7-fluoro-1H-indol-3-yl)-ethanone 7-fluoro-1H-indole-3-carbaldehyde 7-fluoro-1-phenylsulfonyl-1H-indole

N-Boc-2-氟苯胺置于bis-Triphenylphosphine-Palladium(II) Chloride,Copper(L) Iodide,Potassium Tert-Butylate,叔丁基锂,三乙胺体系中,用 四氢呋喃,叔丁醇,正戊烷 作为反应溶剂,化学反应 13.0H,反应生成 7-氟吲哚
参考文献:寻求简单性和灵活性:合理获取 12 种氟代吲哚羧酸
标题:寻求简单性和灵活性:合理获取 12 种氟代吲哚羧酸
摘要:所有十二个在苯并环上带有氟取代基和羧基的吲哚羧酸已经被制备出来.直接来自相应的氟吲哚或氯化衍生物.通过氢/金属置换("金属化"),或通过卤素/金属置换从溴或碘氟吲哚中提取,有机金属中间体每次都被二氧化碳捕获.在大多数情况下,尽管不是所有情况,五元环中的氮原子必须由三烷基甲硅烷基保护.一些溴或碘氟吲哚成功地经受了重卤素的碱性梯度驱动的选择性迁移.在通往目标化合物的途中意外发现.是 5-氟-N-(三烷基甲硅烷基)吲哚的严格位点选择性金属化(4-位的独家去质子化).氟吲哚虽然以前是已知的,但可以使用 Bartoli 或 Leimgruber-Batcho 方法从适当取代的硝基苯中更方便地获得.精心设计了一种新的非常有吸引力的吲哚合成,包括 N-酰基保护的苯胺的邻位锂化,然后是邻位甲酰化,Wittig 氯亚甲基化和碱催化环化,并伴有脱氯化氢.这五个连续的步骤可以简化为一个方便的一锅协议.[在 Scifinder
DOI:10.1002/ejoc.200600118

专利信息

专利号:US-10570114-B2
优先权日:2016-05-19
标题:Synthesis of 6-aryl-4-aminopicolinates and 2-aryl-6-aminopyrimidine-4-carboxylates by direct suzuki coupling
发明人：FISK JASON S; LI XIAOYONG; Muehlfeld Mark; BAUMAN ROBERT S; OPPENHEIMER JOSSIAN; TU SIYU; NITZ MARK A; CHAKRABARTI REETAM; FEIST SHAWN D; RINGER JAMES W; LENG RONALD B
权利人:DOW AGROSCIENCES LLC
摘要:Improved methods of synthesizing 6-aryl-4-aminopicolinates, such as arylalkyl and alkyl 4-amino-3-chloro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates and arylalkyl and alkyl 4-amino-3-chloro-5-fluoro-6-(4-chloro-2-fluoro-3-methoxyphenyl)pyridine-2-carboxylates, are described herein. The improved methods include a direct Suzuki coupling step, which eliminates the protection/de-protection steps in the current chemical process, and therefore eliminates or reduces various raw materials, equipment and cycle time as well as modification of other process conditions including use of crude AP, use of ABA-diMe, and varying pH, catalyst concentration, solvent composition, and/or workup procedures. This includes synthesis of 2-aryl-6-aminopyrimidine-4-carboxylates.

专利号:US-2025002518-A1
优先权日:2023-06-16
标 题 :Synthesis of heteroarynes and use thereof
发明人：MATTMILLER ROBERTS COURTNEY COLLEEN; HUMKE JENNA NICOLE; QUINLIVAN ANSEL ANNABEL; BELLI ROMAN GIANCARLO; KARGBO SALLU SO; PLASEK ERIN ELIZABETH
权利人:UNIV MINNESOTA
摘要:Disclosed herein are heterocyclic arynes and methods for preparing the same. Heteroarynes such as 5-membered O- or N-heterocyclic arynes have been considered inaccessible due to ring strain associated with the triple bond. The methods described herein demonstrate that these arynes can be successfully prepared through the utility of pi-backbonding from a transition metal. Synthetic utility of this method has been demonstrated by the facile synthesis and functionalization of heterocycles using these heteroaryne building blocks.

专利号:US-2017081347-A1
优先权日:2014-04-14
标题:Functionalized azaborine compounds and azaborine-containing biarylcarboxamides, and compositions and methods thereof
发明人：LIU SHIH-YUAN; ZHAO PENG; BROWN ALEC NATHANIEL
权利人:THE TRUSTEES OF BOSTON COLLEGE
摘要:The invention provides novel azaborine compounds, methods for their syntheses and functionalization, and various applications thereof. For example, novel azaborine-containing biarylcarboxylic acids and biarylcarboxamides are disclosed herein, which provide the opportunity to be used as therapeutic agents in different diseases. The novel azaborine-containing compounds show unique physical and biological properties when compared to their corresponding all-carbon compounds. Also, disclosed herein are substituted 1,2-dihydro-1,2-azaborine compounds and methods for making the same including methods for the preparation of various substituted azaborines including alkyl, alkenyl, aryl, nitrile, heteroaryl, and fused ring substituents in the presence of B—H, B—Cl, B—O and N—H bonds from Br-substituted azaborines as well as the synthesis of new fused BN-heterocycles.

专利号:US-9549921-B2
优先权日:2013-06-24
标 题:Heterocyclic compounds and methods of use thereof for the treatment of hepatitis C
发明人：HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD
权利人:HE SHUWEN; LAI ZHONG; DAI XING; XIAO DONG; LONDON CLARE; ZORN NICOLAS; NARGUND RAVI; PALANI ANANDAN; MCCOMAS CASEY C; LI PENG; PENG XUANJIA; SOLL RICHARD; MERCK SHARP & DOHME
摘要:The present invention relates to compounds of formula I that are useful as hepatitis C virus (HCV) NS5B polymerase inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5B polymerase activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.(I)

专利号:US-2018334444-A1
优先权日:2016-05-19
标 题:Synthesis of 6-aryl-4-aminopicolinates and 2-aryl-6-aminopyrimidine-4-carboxylates by direct suzuki coupling

专利号:US-2023357155-A1
优先权日:2020-03-18
标 题:Improved synthesis of 4-amino-6-(heterocyclic)picolinates
发明人：CANTURK BELGIN; DEVARAJ JAYACHANDRAN; HAZARI AMARUKA; KASSL CHRISTOPHER; LEE MELISSA; LI FANGZHENG; LOWE CHRISTIAN T; SIDDALL THOMAS L; WHITEKER GREGORY T; ZHANG CHUNMING
权利人:CORTEVA AGRISCIENCE LLC
摘要:The present disclosure relates to improved processes for preparing 4-amino-6-(heterocyclic)picolinates.