CAS: 348-40-3; 6-Fluorobenzo[d]Thiazol-2-Amine

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1-(4-氟苯基)-2-硫脲置于溴体系中,用 二氯甲烷 用作溶剂,化学反应生成2-氨基-6-氟苯并噻唑
参考文献:新型1-(1,3-苯并噻唑-2-基)-3-氯-4H-螺环[氮杂环丁烷-2,3'-吲哚]-2',4(1'H)-的设计,合成及抗菌研究二酮通过酮-亚胺环加成反应
标题:新型1-(1,3-苯并噻唑-2-基)-3-氯-4H-螺环[氮杂环丁烷-2,3'-吲哚]-2',4(1'H)-的设计,合成及抗菌研究二酮通过酮-亚胺环加成反应
摘要:本研究涉及新型的1-(1,3-苯并噻唑-2-基)-3-氯-4Hspiro [氮杂环丁烷-2,3'-吲哚]-2',4(1'H)-二酮的合成3-(1,3-苯并噻唑-2-Ylimino)-1,3-二氢-2H-吲哚-2-酮衍生物与氯乙酰氯在三乙胺(tea)存在下反应的衍生物.该机制涉及通过形成席夫碱的简单酸或碱催化反应,然后通过乙烯酮-亚胺环加成反应进行环化.所有合成的化合物均通过ft-Ir,1H-NMR,13C-NMR和元素分析进行表征.通过micro Broth Dilution方法检测了合成的衍生物5A-5G对枯草芽孢杆菌,金黄色葡萄球菌,大肠杆菌,铜绿假单胞菌和白色念珠菌菌株的抗菌活性,以测定mic值.氨苄西林 使用micro Broth Dilution方法检查合成化合物的抗菌活性的mic值.发现化合物5A,5B和5C对大肠杆菌(mtcc 442)和铜绿假单胞菌(mtcc 441)
Doi:10.2174/1570178616666190705153224

专利信息

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-7405310-B2
优先权日:2001-03-05
标 题:Non-nucleoside reverse transcriptase inhibitors
发明人：LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA
权利人:MEDIVIR AB
摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.

专利号:US-6562844-B2
优先权日:1998-01-23
标 题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-6417195-B1
优先权日:1999-02-22
标题 :Isoquinoline derivatives and isoquinoline combinatorial libraries
发明人：LEBL MICHAL
权利人:LION BIOSCIENCE AG
摘要:The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinoline derivatives as well as novel libraries comprised of such compounds.

专利号:US-5874443-A
优先权日:1995-10-19
标 题:Isoquinoline derivatives and isoquinoline combinatorial libraries
发明人：KIELY JOHN S; GRIFFITH MICHAEL C
权利人:TREGA BIOSCIENCES INC
摘要:The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinolines as well as novel libraries comprised of many such compounds, and methods of synthesizing the libraries.

专利号:US-7002020-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.