📜N1-Iodomethyluracil置于sodium Tetrahydroborate体系中,用 乙醇 作为反应溶剂,化学反应 6.0H,以64%的收率获得产物1-甲基尿嘧啶 参考文献:Studies On Uracil Derivatives And Analogs Vii. Synthesis Ofn 1-Lodomethyl Derivatives Of Uracil And Dihydrouracil 标题:Studies On Uracil Derivatives And Analogs Vii. Synthesis Ofn 1-Lodomethyl Derivatives Of Uracil And Dihydrouracil 摘要: DOI:10.1055/s-1985-31199
专利信息
专利号:WO-9517903-A1 优先权日:1993-12-28 标 题:Modular design and synthesis of oxazolone-derived molecules 发明人:HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 权利人:ARQULE PARTNERS L P; HOGAN JOSEPH C JR; CASEBIER DAVID; FURTH PAUL; TU CHENG 摘要:The design and synthesis of novel oxazolone-derived molecular modules and the use of the modules in the construction of new molecules and fabricated materials is disclosed. The new molecules and fabricated materials are molecular recognition agents useful in the design and synthesis of drugs, and have applications in separations and materials science.
专利号:US-7122693-B2 优先权日:1988-04-11 标题 :Acetaldehyde acetal compounds, their synthesis, and uses thereof 发明人:BELLEAU EXECUTRIX OF ESTATE PI; DIXIT DILIP M; NGUYEN-BA NGHE 权利人:SHIRE BIOCHEM INC 摘要:The acetaldehyde compounds, 2-thiobenzoylacetaldehyde diethylacetal, 2-benzoyloxyacetaldehyde bis(2-methoxyethyl)acetal, 2-hydroxyacetaldehyde bis( 2-methoxyethyl)acetal, 2-thiobenzoylacetaldehyde bis(2-methoxy-ethyl)acetal, and 2-thioacetaldehyde bis(2-methoxyethyl)acetal, are useful as intermediates in the synthesis of substituted 1,3-oxathiolanes and substituted 1,3-dioxolanes.
专利号:US-2023212204-A1 优先权日:2020-01-16 标题:Reagents and their use for modular enantiodivergent synthesis of c-p bonds 发明人:XU DONGMIN; RIVAS-BASCÓN NAZARET; KNOUSE KYLE W; PADIAL NATALIA; ZHENG BIN; VANTOUROUT JULIEN; SCHMIDT MICHAEL; EASTGATE MARTIN D; BARAN PHI 权利人:BRISTOL MYERS SQUIBB CO; SCRIPPS RESEARCH INST 摘要:The disclosure describes chiral P(V)-based reagents and their uses for the modular, scalable, and stereospecific synthesis of chiral phosphines, phosphine oxides and particular oligonucleotides.
专利号:US-4849513-A 优先权日:1983-12-20 标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups 发明人:SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J 权利人:CALIFORNIA INST OF TECHN 摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.
专利号:US-5118802-A 优先权日:1983-12-20 标 题:DNA-reporter conjugates linked via the 2' or 5'-primary amino group of the 5'-terminal nucleoside 发明人:SMITH LLOYD M; FUNG STEVEN; KAISER JR ROBERT J 权利人:CALIFORNIA INST OF TECHN 摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.
专利号:US-2021220331-A1 优先权日:2016-05-03 标题:Inhibitors of ires-mediated protein synthesis 发明人:GERA JOSEPH F; LICHTENSTEIN ALAN; JUNG MICHAEL E; LEE JIHYE; HOLMES BRENT; BENAVIDES-SERRATO ANGELICA 权利人:UNIV CALIFORNIA; THE UNITED STATE GOVERNMENT REPRESENTED BY THE DEPT OF VETERANS AFFAIRS 摘要:This disclosure relates to inhibitors of IRES-mediated protein synthesis, compositions comprising therapeutically effective amounts of these compounds, and methods of using those compounds and compositions in treating hyperproliferative disorders, e.g., cancers. This disclosure also relates to compositions comprising inhibitors of IRES-mediated protein synthesis and mTOR inhibitors, and to methods of treating cancer by conjoint administration of inhibitors of IRES-mediated protein synthesis and mTOR inhibitors.
[参考文献]: A Le, Et Al. Modeling Of Reaction Steps Relevant To Deoxyuridylate (Dump) Enzymatic Methylation And Thymidylate Synthase Mechanism-Based Inhibition. J Biomol Struct Dyn. 1998 Feb;15(4):703-15. [参考文献]: Bram Boeckx, Et Al. Simulating The Interaction Between Amino Acids And Dna: A Combined Matrix-Isolation Ft-Ir And Theoretical Study Of The 1-Methyluracil·glycine H-Bond Complexes Using A Dual Sublimation Furnace. J Phys Chem B. 2012 Oct 4;116(39):11890-8. [参考文献]: Charles A Lewis Jr, Et Al. Orotic Acid Decarboxylation In Water And Nonpolar Solvents: A Potential Role For Desolvation In The Action Of Omp Decarboxylase. Biochemistry. 2009 Sep 15;48(36):8738-45. [参考文献]: Marek Boczar, Et Al. Theoretical And Spectroscopic Study Of Infrared Spectra Of Hydrogen-Bonded 1-Methyluracil Crystal And Its Deuterated Derivative. J Chem Phys. 2008 Apr 28;128(16):164506. [参考文献]: N N Malinovsky, Et Al. Assessment Of Hepatic Tissue Blood Flow With 133Xe Clearance Technique. Int J Nucl Med Biol. 1981;8(1):77-84.
合成参考文献
摘要:P. A. Levene, L. W. Bass, and H. S. Simms. J. Biol. Chem. 70, 229 (1926). 摘要:K. Nakanishi, N. Suzuki and F. Yamazaki, Bull. Chem. Soc. Jpn. 34, 53 (1961). 摘要:J. Jonas and J. Gut, Collect. Czech. Chem. Commun. 27, 716 (1962). 摘要:J. Gut, M. Prystas, J. Jonas and F. Sorm, Collect. Czech. Chem. Commun. 26, 974 (1961). 参考文献:10.1107/s0108768191013319 摘要:Klooster WT, Swaminathan S, Nanni R, Craven BM. Electrostatic properties of 1-methyluracil from diffraction data. Acta Crystallogr B. 1992 Apr 01;48 ( Pt 2)():217–27. doi: 10.1107/s0108768191013319.