专利号:WO-9407900-A1 优先权日:1992-09-25 标 题 :Synthesis of n-glycosylated compounds with the use of a mild, iodine-catalyzed reaction 发明人:KOREEDA MASATO; HOUSTON TODD A 权利人:UNIV MICHIGAN 摘要:The invention concerns N-glycosylated derivatives of nitrogen nucleophile compounds. The invention also concerns a mild, cost effective, stereoselective, regioselective, and generally applicable method for the preparation of N-glycosides by N-glycosylation of azide and amide nucleophile compounds. The method employs iodine in a catalytic amount that uniquely does not pose an environmental hazard. The invention provides efficient access to key intermediates for the synthesis inter alia of analogs of AZT and DDI and for the synthesis of conventional N-nucleoside antibiotic drugs and their novel N-glycosylated analogs.
专利号:US-8314209-B2 优先权日:2007-12-12 标 题 :Lipid-assisted synthesis of polymer compounds and methods for their use 发明人:RAJAMANI SUDHA; OLASAGASTI FELIX; DEAMER DAVID W; BENNER SEICO 权利人:RAJAMANI SUDHA; OLASAGASTI FELIX; DEAMER DAVID W; BENNER SEICO; UNIV CALIFORNIA 摘要:The invention herein disclosed provides for methods for the synthesis of polymers from monomers. In particular the method provides for the synthesis of polynucleotides from mononucleotides in the absence of catalytic enzymes. The method comprises providing an aqueous solution having a plurality of phospholipid molecules and monomer molecules; subjecting the aqueous solution to fluctuating temperature conditions; subjecting the aqueous solution to fluctuating cycles of drying and hydrating conditions; subjecting the aqueous solution to fluctuating [H + ] conditions; the fluctuating conditions thereby allowing formation of a chemical bond between at least two monomers to create a polymer. The invention is of particular use in the fields of molecular biology, structural biology, cell biology, molecular switches, molecular circuits, and molecular computational devices, and the manufacture thereof.
专利号:US-2003162992-A1 优先权日:2001-12-14 标 题 :Preparation of intermediates useful in the synthesis of antiviral nucleosides 发明人:WATANABE KYOICHI A; DU JINFA 摘要:The present invention is an efficient process for the manufacture of α-acyloxyacetaldehyde, a key intermediate in the synthesis of 1,3-oxathiolane and 1,3-dioxolane nucleosides.
专利号:US-6005097-A 优先权日:1996-06-14 标题 :Processes for high-yield diastereoselective synthesis of dideoxynucleosides 发明人:CHEN SHU-HUI; LI XIUYAN 权利人:VION PHARMACEUTICALS INC 摘要:The present invention relates to methods for substantially enhancing the stereoselective synthesis of β-anomeric nucleoside analogs. In methods according to the present invention, the introduction of a phenylseleno group onto a blocked lactone sugar precursor may be selected so that the desirable phenylseleno substituent is introduced on the side of the blocked lactone away from the blocking group. This stereospecific introduction of the phenylseleno group in sugar precursor allows the synthesis of nucleoside analogs and in particular, 2',3',-dideoxy- and 2',3'-dideoxy-2',3'-didehydronucleoside analogs in very high yield. In certain preferred embodiments, the preferred phenylseleno blocked lactone is obtained in an amount representing approximately 90% or more of the total amount of the stereoisomers obtained. In even more preferred embodiments, the amount of the preferred stereoisomer is at least 95%, even more preferably at least about 97% of the total amount of phenylseleno blocked lactone produced.
专利号:US-9206209-B2 优先权日:2010-10-19 标 题:Nucleotide analogue, method of synthesis of nucleotide analogue, use of nucleotide analogue, antiviral pro-nucleotide, pharmaceutical composition 发明人:KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ 权利人:KRASZEWSKI ADAM; ROMANOWSKA JOANNA; SOBKOWSKI MICHAL; SZYMANSKA-MICHALAK AGNIESZKA; STAWINSKI JACEK; BORYSKI JERZY; LIPNIACKI ANDRZEJ; PIASEK ANDRZEJ; INST CHEMII BIOORG PAN; NARODOWY INST LEKOW 摘要:An exemplary emboidment is related to a pharmaceutical composition of the class of nucleotide analogues and antiviral pro-nucleotides useful in partial or complete inhibition of human immunodeficiency virus (HIV). An exemplary embodiment is expressed in the formula (XVI): n nwhere X stands for N 3 and B stands for thymidine-1-yl, or X stands for H and B stands for uracil-1-yl or adenin-1-yl or hypoxanthin-1-yl.A method of synthesis of the nucleotide analogue using a phosphorylating agent for synthesis of the nucleotide analogue is provided.
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.
1: Pavia-Ruz N, Rossouw M, Sáez-Llorens X, Bunupuradah T, Taylor M, Yang R, Sevinsky H, Krystal M, Lataillade M, Seekins D, Biguenet S. Efavirenz Capsule Sprinkle and Liquid Formulations with Didanosine and Emtricitabine in HIV-1-Infected Infants and Children 3 Months to 6 Years of Age: Study AI266-922. Pediatr Infect Dis J. 2015 Sep 15. [Epub ahead of print] doi: 10.14309/crj.2015.24. eCollection 2015 Jan. 3: Cunha RD, Abreu CM, Sousa AK, Mabombo VC, Nijhuis M, de Jong D, Tanuri A. Short Communication: In Vitro Accumulation of Drug Resistance Mutations in Chimeric Infectious Clones Containing Subtype B or C Reverse Transcriptase and Selected with Tenofovir or Didanosine. AIDS Res Hum Retroviruses. 2015 Aug;31(8):851-8. doi: 10.1089/AID.2014.0324. Epub 2015 Jul 16. doi: 10.1016/j.biopha.2014.12.047. Epub 2015 Jan 13. doi: 10.1016/j.medcli.2014.09.014. Epub 2014 Dec 13. Spanish. doi: 10.1016/j.colsurfb.2014.09.055. Epub 2014 Oct 6. doi: 10.1177/0956462414554433. Epub 2014 Oct 2. 9: Sun R, Eriksson S, Wang L. Down-regulation of mitochondrial thymidine kinase 2 and deoxyguanosine kinase by didanosine: implication for mitochondrial toxicities of anti-HIV nucleoside analogs. Biochem Biophys Res Commun. 2014 Jul 25;450(2):1021-6. doi: 10.1016/j.bbrc.2014.06.098. Epub 2014 Jun 26. doi: 10.1371/journal.pone.0097067. eCollection 2014.
合成参考文献
摘要:Liang, Y.; Wen, Z.; Cabrera, M.; Howlader, A. H.; Wnuk, S. F., Science of Synthesis Knowledge Updates, (2020) 1, 268. 参考文献:10.1007/s00467-006-0109-3 摘要:Hussain S, Khayat A, Tolaymat A, Rathore MH. Nephrotoxicity in a child with perinatal HIV on tenofovir, didanosine and lopinavir/ritonavir. Pediatr Nephrol. 2006 Jul;21(7):1034–6. doi: 10.1007/s00467-006-0109-3. 参考文献:10.1007/164_2020_383 摘要:Vickneson K, George J. Xanthine Oxidoreductase Inhibitors. Handb Exp Pharmacol. 2021;264():205–28. doi: 10.1007/164_2020_383. 参考文献:10.1208/s12248-021-00675-w 摘要:Murata Y, Neuhoff S, Rostami-Hodjegan A, Takita H, Al-Majdoub ZM, Ogungbenro K. In Vitro to In Vivo Extrapolation Linked to Physiologically Based Pharmacokinetic Models for Assessing the Brain Drug Disposition. The AAPS Journal. 2022 Jan 13;24(1):28. doi: 10.1208/s12248-021-00675-w. 参考文献:10.2165/00019053-200422010-00004 摘要:Tramarin A, Campostrini S, Postma MJ, Calleri G, Tolley K, Parise N, de Lalla F; Palladio Study Group. A multicentre study of patient survival, disability, quality of life and cost of care: among patients with AIDS in northern Italy. Pharmacoeconomics. 2004;22(1):43–53. doi: 10.2165/00019053-200422010-00004.