2-氨基腺嘌呤核苷置于吡啶,Potassium Nitrite,氢氟酸,Calcium Carbonate体系中,用 水 用作溶剂,化学反应 2.0H,反应生成2-氟腺苷 参考文献:Novel Chemical Agents Comprising An Adenosine Moiety Or An Adenosine Analog Moiety And An Imaging Moiety And Methods Of Their Use 标题:Novel Chemical Agents Comprising An Adenosine Moiety Or An Adenosine Analog Moiety And An Imaging Moiety And Methods Of Their Use 摘要:本发明涉及新型化合物的化学试剂及其用于心肌灌注成像的用途.该发明还涉及用于制备这种新型试剂的试剂盒.本发明的化学试剂包括(a)腺苷类似物基团或腺苷基团,以及(b)成像基团.
专利号:US-2020239921-A1 优先权日:2016-02-03 标 题 :Chemoenzymatic synthesis of s-nucleosyl amino acids (sna), analogs of s-adenosyl-l-methionine and s-adenosyl-l- homocysteine and uses thereof 发明人:BURGOS EMMANUEL SEBASTIEN; SHECHTER DAVID 权利人:ALBERT EINSTEIN COLLEGE MEDICINE 摘要:Disclosed are methods for chemoenzymatic synthesis of S-Nucleosyl Amino acid probes (SNA), analogs of S-adeno-syl-L-methionine and S-adenosyl-L-homo-cysteine, analogs synthesized by the methods, and uses thereof.
专利号:US-6175004-B1 优先权日:1998-09-01 标题 :Process for the synthesis of oligonucleotides incorporating 2-aminoadenosine 发明人:ROSS BRUCE S; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:This invention presents novel processes for incorporating 2-aminoadenosine and 2-aminoadenosine analogs into oligonucleotides. A halogenated adeninosine is incorporated into an oligonucleotide using standard synthesis methods, such as phosphoramidited protocols. Subsequent reaction with an amine results in the desired product. The oligonucleotides produced provide stronger hybridization to their target sequences. These oligonucleotides can be useful compounds, inter alia for diagnostic and therapeutic applications.
专利号:US-2005080260-A1 优先权日:2003-04-22 标 题 :Preparation of prodrugs for selective drug delivery 发明人:MILLS RANDELL L; WU GUO-ZHANG 摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.
专利号:US-8859522-B2 优先权日:2011-04-27 标题:Processes for the preparation of regadenoson and a new crystalline form thereof 发明人:WOOLDRIDGE LUZVIMINDA T; MA CHUN; NADJI SOURENA 权利人:WOOLDRIDGE LUZVIMINDA T; MA CHUN; NADJI SOURENA; RELIABLE BIOPHARMACEUTICAL CORP 摘要:This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described.
专利号:US-9771390-B2 优先权日:2013-12-10 标题:Process for the preparation of regadenoson 发明人:ZHANG XIAOHENG; MEI LIJUN 权利人:SCINOPHARM TAIWAN LTD 摘要:The present invention provides novel processes for the preparation of regadenoson having the formula (I). In some embodiments, the intermediates for the synthesis of regadenoson are also provided.
专利号:US-8614312-B2 优先权日:2008-02-21 标 题 :Method for preparing nucleotides and related analogues by synthesis on soluble substrate, and biological tools thus prepared 发明人:PEYROTTES SUZANNE; PERIGAUD CHRISTIAN; CRAUSTE CELINE 权利人:PEYROTTES SUZANNE; PERIGAUD CHRISTIAN; CRAUSTE CELINE; CENTRE NAT RECH SCIENT; UNIV MONTPELLIER II 摘要:The invention concerns a method for preparing monomer nucleotides or nucleotide analogues comprising the steps of: (1) coupling a soluble polyethylene glycol support provided with at least one diacid or ether-acid linker and a monomer nucleoside or nucleoside analogue to an amine group or hydroxyl group of the nucleoside with the aid of a coupling agent; (2) at least one step for phosphorylation of said nucleoside or nucleoside analogue coupled to said support with a phosphorylation agent; (3) cleavage of said support and recovery of at least one monomer nucleotide or nucleotide analogue. The nucleotides prepared are biological tools.
1: Ye S, Rezende MM, Deng WP, Herbert B, Daly JW, Johnson RA, Kirk KL. Synthesis of 2',5'-dideoxy-2-fluoroadenosine and 2',5'-dideoxy-2,5'-difluoroadenosine: potent P-site inhibitors of adenylyl cyclase. J Med Chem. 2004 Feb 26;47(5):1207-13. doi: 10.1021/jm0303599. 251(21):6757-66. 22(10):1899-905. doi: 10.1081/NCN-120025237. 10:474-84. 87(3):825-30. doi: 10.1093/oxfordjournals.jbchem.a132812. 35(2):210-4. Russian. doi: 10.1134/s1068162009020071. 10(6):1165-6. doi: 10.1021/jm00318a042. 266(4 Pt 2):H1596-603. doi: 10.1152/ajpheart.1994.266.4.H1596. 26(10-12):1543-6. doi: 10.1080/15257770701545218. 6(3):133-43. doi: 10.1002/tcr.20078. (50):1-2. doi: 10.1093/nass/nrl001. 31(22):3713-6. doi: 10.1016/0006-2952(82)90608-6. 11(4):539. doi: 10.3390/biom11040539. 14: Gao ZG, Jacobson KA. Partial agonists for A(3) adenosine receptors. Curr Top Med Chem. 2004;4(8):855-62. doi: 10.2174/1568026043450989.
合成参考文献
摘要:National Cancer Institute Screening Program Data Summary, Developmental Therapeutics Program., JAN1986 摘要:Progress in Medical Chemistry., 7(69), 1970 [] 参考文献:10.2165/00003495-199400476-00006 摘要:Plunkett W, Gandhi V. Evolution of the arabinosides and the pharmacology of fludarabine. Drugs. 1994;47 Suppl 6():30–8. doi: 10.2165/00003495-199400476-00006.