5-氟-2'-脱氧脲核苷置于4-二甲氨基吡啶,Ammonium Hydroxide,三氯氧磷体系中,用 吡啶 用作溶剂,化学反应生成5-氟脱氧胞苷 参考文献:Synthesis Of An Oligonucleotide Suicide Substrate For Dna Methyltransferases 标题:Synthesis Of An Oligonucleotide Suicide Substrate For Dna Methyltransferases 摘要:The Large-Scale Chemical Synthesis Of An Oligodeoxynucleotide Containing 5-Fluoro-2'-Deoxycytidine (Fdc) And Its Characterization Are Described. The Fdc Residue Is Introduced Via The Corresponding 4-O-(2,4,6-Trimethylphenyl)-2'-Deoxyuridine Derivative,Which Undergoes Clean Conversion To Fdc During Removal Of The Oligonucleotide Protecting Groups With Ammonia. A Double-Stranded Oligodeoxynucleotide Containing Fdc Inactivated The Dna Methyltransferase Enzyme M.Hae Iii By Irreversible Formation Of A Covalent Protein-Dna Complex. Doi:10.1021/jo00037A006
专利号:US-11858953-B2 优先权日:2018-04-04 标 题:Compositions and methods for synthesis of phosphorylated molecules 发明人:CHAPUT JOHN; LIAO JEN-YU; BALA SAIKAT 权利人:UNIV CALIFORNIA 摘要:The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates.
专利号:US-5663323-A 优先权日:1993-02-23 标题 :Synthesis of 4-alkoxy-5-fluoro-2'-deoxyuridine and its incorporation into oligonocleotides 发明人:SOWERS LAWRENCE C 权利人:HOPE CITY 摘要:A synthesis of 5-fluoro-2'-ideoxycytidine, of oligonucleotides containing 5-fluoro-2'-deoxycytidine and of certain novel 4-alkoxy-5-fluoro-2'-deoxyuridines is disclosed. These 4-alkoxy compounds are useful intermediates for the preparation of other 4-substituted, 5-fluoro pyrimidine deoxynucleosides, and spontaneously hydrolyze in target cells to form FdU and derivatives thereof.
专利号:US-9605261-B2 优先权日:2008-09-06 标 题:RNA synthesis—phosphoramidites for synthetic RNA in the reverse direction, and application in convenient introduction of ligands, chromophores and modifications of synthetic RNA at the 3′-end 发明人:SRIVASTAVA SURESH C; PANDEY DIVYA; BAJPAI SATYA P; SRIVASTAVA NAVEEN P 权利人:CHEMGENES CORP 摘要:The present invention relates to novel phosphoramidites, A-n-bz, C-n-bz, C-n-ac, G-n-ac and U are produced with an HPLC purity of greater than 98% and 31 P NMR purity greater than 99%. A novel process of reverse 5′→3′ directed synthesis of RNA oligomers has been developed and disclosed. Using that method demonstrated high quality RNA synthesis with coupling efficiency approaching 99%.
专利号:US-2022363662-A1 优先权日:2021-04-20 标题 :Compounds as lxr agonists 发明人:PUJALA BRAHMAM; SATHE BALAJI DASHRATH; DANODIA ABHINANDAN; GUPTA ASHU; SONI SANJEEV; KUMAR VIVEK; ANSARI AMANTULLAH; KHAN FARHA; SARKAR ARINDAM; PAYGHAN PAVAN V 权利人:INTEGRAL BIOSCIENCES PRIVATED LTD 摘要:The present invention generally discloses compounds having LXR (the liver X receptor) agonistic activity, to the use of such compounds in the treatment of various disorders such as proliferative disorders, Alzheimer's disease, inflammatory diseases, and diseases characterized by defects in cholesterol and lipid metabolism. Specifically, the present invention discloses compound of formula (IA) which exhibit LXR agonist activity, specifically to LXRβ. The invention also discloses method of synthesis of said compounds, method of using said compounds, pharmaceutical compositions comprising said compounds and method of using thereof.
专利号:US-2020239500-A1 优先权日:2018-04-04 标 题 :Compositions and Methods for Synthesis of Phosphorylated Molecules
专利号:EP-3686190-A1 优先权日:2013-07-11 标 题 :Synthesis of therapeutically active compounds
1: Holleran JL, Eiseman JL, Parise RA, Kummar S, Beumer JH. LC-MS/MS assay for the quantitation of FdCyd and its metabolites FdUrd and FU in human plasma. J Pharm Biomed Anal. 2016 Sep 10;129:359-66. doi: 10.1016/j.jpba.2016.07.027. 2: Beumer JH, Parise RA, Newman EM, Doroshow JH, Synold TW, Lenz HJ, Egorin MJ. Concentrations of the DNA methyltransferase inhibitor 5-fluoro-2'-deoxycytidine (FdCyd) and its cytotoxic metabolites in plasma of patients treated with FdCyd and tetrahydrouridine (THU). Cancer Chemother Pharmacol. 2008 Jul;62(2):363-8. doi: 10.1007/s00280-014-2674-7. 4: Holleran JL, Beumer JH, McCormick DL, Johnson WD, Newman EM, Doroshow JH, Kummar S, Covey JM, Davis M, Eiseman JL. Oral and intravenous pharmacokinetics of 5-fluoro-2'-deoxycytidine and THU in cynomolgus monkeys and humans. Cancer Chemother Pharmacol. 2015 Oct;76(4):803-11. doi: 10.1007/s00280-015-2857-x.
合成参考文献
摘要:Advances in Teratology., 3(181), 1968 参考文献:10.1038/sj.cdd.4400999 摘要:Tombal B, Denmeade SR, Gillis JM, Isaacs JT. A supramicromolar elevation of intracellular free calcium ([Ca(2+)](i)) is consistently required to induce the execution phase of apoptosis. Cell Death Differ. 2002 May;9(5):561–73. doi: 10.1038/sj.cdd.4400999. 参考文献:10.1093/nar/23.21.4275 摘要:Shen JC, Zingg JM, Yang AS, Schmutte C, Jones PA. A mutant HpaII methyltransferase functions as a mutator enzyme. Nucleic Acids Res. 1995 Nov 11;23(21):4275–82. 参考文献:10.1007/s00294-002-0296-9 摘要:Kurtz JE, Exinger F, Erbs P, Jund R. The URH1 uridine ribohydrolase of Saccharomyces cerevisiae. Curr Genet. 2002 Jun;41(3):132–41. doi: 10.1007/s00294-002-0296-9. 参考文献:10.1208/s12249-010-9383-2 摘要:Guo D, Myrdal PB, Karlage KL, O’Connell SP, Wissinger TJ, Tabibi SE, Yalkowsky SH. Stability of 5-Fluoro-2′-deoxycytidine and Tetrahydrouridine in Combination. AAPS PharmSciTech. 2010 Feb 12;11(1):247–52. doi: 10.1208/s12249-010-9383-2.