2-脱氧-4-C-乙炔-2-氟腺苷酸置于4-二甲氨基吡啶体系中,用32.9%的收率获得产物双(五氟苯基)碳酸 参考文献:Adenosine Derivative And Pharmaceutical Composition Comprising The Same 标题:Adenosine Derivative And Pharmaceutical Composition Comprising The Same 摘要:本文披露了腺苷衍生物前药及其组合物,可用于治疗hiv感染或rna病毒感染.
专利号:US-2008125587-A1 优先权日:2006-05-25 标 题 :Synthesis of triazole compounds that modulate HSP90 activity 发明人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 权利人:CHIMMANAMADA DINESH U; LEE CHI-WAN; JAMES DAVID; ZHANG SHIJIE; YING WEIWEN; CHAE JUNGHYUN; PRZEWLOKA TERESA 摘要:The present invention provides novel methods of preparing triazole compounds which inhibit the activity of Hsp90. One embodiment of the invention is directed to methods for preparing a triazole compound represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising the steps of: a) reacting an amide represented by the following Structural Formula: n n n n n n n n n n with a thionation reagent to form a thioamide; b) reacting the thioamide of step a) with hydrazine to form a hydrazonamide; c) reacting the hydrazonamide of step b) with a carbonylation or a thiocarbonylation reagent. n In one embodiment, the present invention is a method of synthesis of a compound of formula (IA) n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof, comprising reacting a compound of formula (IIA) n n n n n n n n n n with an oxidizing agent, thereby producing a compound of formula (IA). n The present invention is also directed to a method of preparing a compound or a tautomer thereof represented by the following Structural Formula: n n n n n n n n n n or a tautomer, a pharmaceutically acceptable salt, solvate, or clathrate, or a prodrug thereof. The method comprises the step of reacting a first starting compound represented by the following Structural Formula: n n n n n n n n n n in the presence of a mercuric salt, with a second starting compound represented by the following Structural Formula:
专利号:US-11034664-B1 优先权日:2020-05-11 标题 :Synthesis of cyclic carbonate monomers 发明人:PARK NATHANIEL H; HEDRICK JAMES L; PIUNOVA VICTORIA A; ARRECHEA PEDRO; ERDMANN TIM 权利人:IBM 摘要:Techniques regarding the synthesis of cyclic carbonate monomers are provided. For example, one or more embodiments described herein can comprise a method, which can include cyclizing a functionalized diol monomer with N,N′-carbonyldiimidazole, wherein the cyclizing produces a cyclic carbonate monomer and an imidazole carbamate. The method can also include activating the imidazole carbamate with an acid, wherein the activating promotes cyclization of the imidazole carbamate into the cyclic carbonate monomer.
专利号:US-11738092-B2 优先权日:2019-12-04 标题:Methods and compositions for synthesis of therapeutic nanoparticles 发明人:WYENT EMILY A; BLUMENFELD CARL M; LAMM ROBERT J 权利人:DANTARI INC 摘要:Improved methods and reactants for the chemical synthesis of therapeutic nanoparticles are provided. The nanoparticles comprise a polymeric core, to which is attached one or more homing molecules and one or more therapeutic agents. Improvements in speed, yield and purity are attained using the methods disclosed herein.
专利号:US-6384210-B1 优先权日:1997-03-20 标题:Solvent for biopolymer synthesis, solvent microdroplets and methods of use 发明人:BLANCHARD ALAN P 权利人:UNIV WASHINGTON 摘要:The present invention provides a method of biopolymer, esp. oligonucleotide, synthesis. The method consists of coupling a first nucleotide to a second nucleotide in a high surface tension solvent. The invention also provides microdroplets of a soln. comprising a solvent having a b.p. of 150 degree. C. or above, a surface tension of 30 dynes/cm or above, and a viscosity of 0.015 g/(cm)(sec), e.g., propylene carbonate. Such microdroplets are useful for the synthesis of chem. species, particularly biopolymers such as oligonucleotides and peptides, as well as arrays of chem. species. An automated system for oligonucleotide synthesis is described, which comprises delivery of microdroplets by inkjet technol. and computer control of the process. The high surface tension solvent used is selected for compatibility with the inkjet technol.
专利号:US-2020354404-A1 优先权日:2019-05-09 标 题 :Peptidomimetic agents, synthesis and uses thereof 发明人:AL-ABED YOUSEF 权利人:FEINSTEIN INSTITUTES FOR MEDICAL RESEARCH 摘要:Compounds for use in synthesis of peptidomimetic agents; synthesis of peptidomimetic agents; peptidomimetic diagnostic and therapeutic agents; and uses of the compounds and peptidomimetic agents in drug discovery, diagnosis, prevention and treatment of diseases are described.
专利号:US-6419883-B1 优先权日:1998-01-16 标题 :Chemical synthesis using solvent microdroplets 发明人:BLANCHARD ALAN P 权利人:UNIV WASHINGTON 摘要:The present invention relates to microdroplets of a solution comprising a solvent having a boiling point of 150° C. or above, a surface tension of 30 dynes/cm or above, and a viscosity of 0.015 g/(cm)(sec). Such microdroplets are useful for the synthesis of chemical species, particularly biopolymers such as oligonucleotides and peptides, as well as arrays of chemical species. Preferably, the solvent has the formula (I):whereinA=O or S;X=O, S or N (C1-C4 alkyl)Y=O, S, N(C1-C4 alkyl) or CH2; andR=C1-C20 straight or branched chain alkyl.
[参考文献]: V A Efimov, Et Al. Dipentafluorophenyl Carbonate--A Reagent For The Synthesis Of Oligonucleotides And Their Conjugates. Nucleic Acids Res. 1993 Nov 25;21(23):5337-44. [参考文献]: V N Medvedkin, Et Al. [参考文献]: Bioorg Khim. 1989 Apr;15(4):460-4.
合成参考文献
参考文献:10.1038/s41428-025-01069-x 摘要:Fukushima K. Degradation technologies for condensation polymers mediated by organic catalysts. Polym J. 2025 Jun 18;57(10):1083–94. doi: 10.1038/s41428-025-01069-x. 参考文献:10.1134/s1070363225606003 摘要:Vigorov AY, Korolyova MA, Levit GL, Krasnov VP. Synthesis and Properties of 4-Amino-5-oxoproline Derivatives (A Review). Russ J Gen Chem. 2026 Feb 24;96(4). doi: 10.1134/s1070363225606003. 参考文献:10.1007/s11030-013-9469-3 摘要:Ahmetaj S, Velikanje N, Grošelj U, Šterbal I, Prek B, Golobič A, Kočar D, Dahmann G, Stanovnik B, Svete J. Parallel synthesis of 7-heteroaryl-pyrazolo[1,5-a]pyrimidine-3-carboxamides. Mol Divers. 2013 Nov;17(4):731–43. doi: 10.1007/s11030-013-9469-3.