2-乙酰氧基-2-甲基丙酸置于氯化亚砜,Lithium Bromide体系中,用 乙酸乙酯 作为反应溶剂,化学反应 4.0H,反应生成 2-乙酰氧基异丁酰溴 参考文献:Nucleotides,Part Lix,Synthesis,Characterization,And Biological Activities Of New Potential Antiviral Agents: (2'-5')Adenylate Trimer Analogs Containing 3'-Deoxy-3'-(Hexadecanoylamino)Adenosine At The 2'-Terminus 标题:Nucleotides,Part Lix,Synthesis,Characterization,And Biological Activities Of New Potential Antiviral Agents: (2'-5')Adenylate Trimer Analogs Containing 3'-Deoxy-3'-(Hexadecanoylamino)Adenosine At The 2'-Terminus 摘要:Based Upon 3'-Amino-3'-Deoxyadenosine (15),Its Protected 3'-Hexadecanoylamino Derivative 22 Was Chosen As Starting Material For The Synthesis Of A Series Of New Modified 2'-5'-Adenylate Trimers 33-36 As Potential Antiviral Agents. All (2'-5')A Trimer Analogs 33-36 Inhibit Hiv-1 Replication As Measured By The Inhibition Of Syncytia Formation And Inhibition Of Hiv-1 Reverse Transcriptase Activity. Compound 34 Inhibits Hiv-1 Reverse Transcription By 100% And Subsequently Inhibits Expression Of Hiv-1 P24. However,Compound 35 Acts Differently,Since It Does Not Inhibit Hiv-1 Reverse Transcription,Hiv-1 Integrase,Or Hiv-1 P24 Expression. Therefore,35 Appears To Exert Its Inhibitory Effect At A Later Stage Of Hiv-1 Replication,I.E.,The Budding Process. DOI:10.1002/(Sici)1522-2675(19990407)82:4<597::Aid-Hlca597>3.0.Co;2-V
专利号:US-7888337-B2 优先权日:2007-08-31 标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG 权利人:ACADEMIA SINICA 摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
专利号:WO-9323413-A1 优先权日:1992-05-13 标 题:Synthesis of nucleotide monomers 发明人:BEIGELMAN LEONID; MATULIC-ACADEMIC JASENKA 权利人:RIBOZYME PHARM INC 摘要:Methods for synthesis of 2',3'-dideoxycytidine, 2',3'-dideoxyguanosine, 2',3'-dideoxyadenosine, 2',3'-dideoxyinosine and 2',3'-dideoxyguanosine, and 3'-O-benzoyl-2'-deoxyribonucleoside.
专利号:US-4900828-A 优先权日:1988-05-12 标 题:Intermediate compounds and an improved procedure for the synthesis of 2',3'-dideoxycytidine 发明人:BELICA PETER S; HUANG TAI-NANG; MANCHAND PERCY S; PARTRIDGE JOHN J; TAM STEVE 权利人:HOFFMANN LA ROCHE 摘要:A method for the synthesis of 2',3'-dideoxycytidine comprising a novel procedure of bromoacetylating cytidine to yield novel intermediates which are subsequently reduced and hydrogenated by novel procedures to yield 2',3'-dideoxycytidine.
专利号:US-9802953-B2 优先权日:2007-10-03 标 题 :Intermediates and methods for the synthesis of halichondrin B analogs 发明人:CHASE CHARLES E; ENDO ATSUSHI; FANG FRANCIS G; LI JING 权利人:EISAI R&D MAN CO LTD 摘要:Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
专利号:US-2004126792-A1 优先权日:2002-09-18 标 题 :Synthesis and applications of trinucleotide pCpCpA-3'-NH-aminoacyl derivatives 发明人:ZHANG BILIANG 摘要:The present invention relates to the synthesis of novel compounds for the inhibition of peptide synthesis in the ribosome. It also relates to improved methods for directly monitoring peptide bond formation in the ribosome. These compounds can be used for high throughput screening of proposed therapeutically active drug species (e.g., antibiotics) targeted to ribosomes.
专利号:US-7109377-B2 优先权日:1996-10-16 标 题:Synthesis of combinatorial libraries of compounds reminiscent of natural products 发明人:SCHREIBER STUART L; SHAIR MATTHEW D; TAN DEREK S; FOLEY MICHAEL A; STOCKWELL BRENT R 权利人:HARVARD COLLEGE 摘要:The present invention provides complex compounds reminiscent of natural products and libraries thereof, as well as methods for their production. The inventive compounds and libraries of compounds are reminiscent of natural products in that they contain one or more stereocenters, and a high density and diversity of functionality. In general, the inventive libraries are synthesized from diversifiable scaffold structures, which are synthesized from readily available or easily synthesizable template structures. In certain embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from a shikimic acid based epoxyol template. In other embodiments, the inventive compounds and libraries are generated from diversifiable scaffolds synthesized from the pyridine-based template isonicotinamide. The present invention also provides a novel ortho-nitrobenzyl photolinker and a method for its synthesis. Furthermore, the present invention provides methods and kits for determining one or more biological activities of members of the inventive libraries. Additionally, the present invention provides pharmaceutical compositions containing one or more library members.