专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:WO-2021014395-A1 优先权日:2019-07-24 标题:Process for the synthesis of deuterated capsaicin, capsaicinoids and synthetic capsaicin analogs 发明人:ORUGANTI SRINIVAS; AMRUTAPU SRAVANTH KUMAR; SAMPATH MAGESH; SEN SAIKAT 权利人:DR REDDY’S INST OF LIFE SCIENCES 摘要:The present application provides novel processes for the synthesis of deuterated intermediates of capsaicinoids, particularly II, III, IV and V of capsaicinoids, relating to pharmaceutical applications. The invention also provides novel intermediates of compounds of formula IX, XIV, XV, XVI, XVII, XVIII, XX and XXI utilized in the process of making deuterated capsaicin II, III, IV and V.
专利号:US-2009171097-A1 优先权日:2005-11-22 标题 :Automated solid phase synthesis of pyrrole-imidazole polyamide 发明人:SUGIYAMA HIROSHI; DOHNO CHIKARA; FUKUDA NOBORU 权利人:SUGIYAMA HIROSHI; DOHNO CHIKARA; FUKUDA NOBORU 摘要:A synthesis method for pyrrole-imidazole polyamide is automated at a higher level and can produce a product with a high yield in a more stable manner. In a solid phase synthesis method, the automated synthesis of a polyimide can be promoted by using HCTU as a condensation-activator, the yield of a product can be increased by charging a monomer in a solid form, and a pyrrole-imidazole polyamide having any sequence can be synthesis by combining the synthesis method with a manual synthesis with an acid chloride.
专利号:WO-2024185734-A1 优先权日:2023-03-03 标 题:Polyphosphorylated nucleoside, phosphate-activated nucleotide used for synthesis of polyphosphorylated nucleoside and method for synthesis of same, and method for synthesis of polyphosphorylated nucleoside using phosphate-activated nucleotide 发明人:KATAOKA MASANORI; FUKUI CHIHARU; TSUJI YOHEI; FUJIMURA Kazuma 权利人:NATIAS INC 摘要:The present invention provides: a polyphosphorylated nucleoside which has a structure represented by formula (I) and can be efficiently produced by a short process and a simple operation with use of a less expensive material; a phosphate-activated nucleotide which is used for the synthesis of the polyphosphorylated nucleoside and a method for the synthesis of this phosphate-activated nucleotide; and a method for the synthesis of a polyphosphorylated nucleoside using a phosphate-activated nucleotide. In the formula, B represents a protected or unprotected, natural or artificial nucleoside base; R 1 , R 2 , R 4 and R 5 each represent H or an alkyl group or the like, and R 1 , R 2 , R 4 and R 5 may be the same as or different from each other; X and Y each represents H, OH, OCH 3 or the like; h represents an integer of 1 to 3; p, n, m and q each represent 0 or an integer, and p, n, m and q are in no particular order; and (p + n + m + q) is an integer of 0 to 5,000.
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
[参考文献]: Chancievan Thangaratnarajah, Et Al. Calcium-Induced Conformational Changes Of The Regulatory Domain Of Human Mitochondrial Aspartate/glutamate Carriers. Nat Commun. 2014 Nov 20:5:5491. [参考文献]: Debashree Basudhar, Et Al. Analysis Of Cytochrome P450 Cyp119 Ligand-Dependent Conformational Dynamics By Two-Dimensional Nmr And X-Ray Crystallography. J Biol Chem. 2015 Apr 17;290(16):10000-17. [参考文献]: Georgina Kerr, Et Al. A Small Molecule Targeting Alk1 Prevents Notch Cooperativity And Inhibits Functional Angiogenesis. Angiogenesis. 2015 Apr;18(2):209-17. [参考文献]: Hossein Asgarian-Omran, Et Al. Interaction Of Bordetella Pertussis Filamentous Hemagglutinin With Human Tlr2: Identification Of The Tlr2-Binding Domain. Apmis. 2015 Feb;123(2):156-62. [参考文献]: Juliana Fattori, Et Al. Rxr Agonist Modulates Tr: Corepressor Dissociation Upon 9-Cis Retinoic Acid Treatment. Mol Endocrinol. 2015 Feb;29(2):258-73.
合成参考文献
参考文献:10.1007/s10529-010-0224-x 摘要:Yeom SJ, Kim BN, Park CS, Oh DK. Substrate specificity of ribose-5-phosphate isomerases from Clostridium difficile and Thermotoga maritima. Biotechnol Lett. 2010 Jun;32(6):829–35. doi: 10.1007/s10529-010-0224-x. 参考文献:10.1007/s10266-009-0118-3 摘要:Niimi M, Firth NA, Cannon RD. Antifungal drug resistance of oral fungi. Odontology. 2010 Feb;98(1):15–25. doi: 10.1007/s10266-009-0118-3. 参考文献:10.18632/aging.100017 摘要:Gertz M, Fischer F, Leipelt M, Wolters D, Steegborn C. Identification of Peroxiredoxin 1 as a novel interaction partner for the lifespan regulator protein p66Shc. Aging (Albany NY). 2009 Jan 30;1(2):254–65. 参考文献:10.4110/in.2009.9.4.138 摘要:Park HJ, Kim JY, Jung KI, Kim TJ. Characterization of a Novel Gene in the Extended MHC Region of Mouse, NG29/Cd320, a Homolog of the Human CD320. Immune Netw. 2009 Aug;9(4):138–46. 参考文献:10.4110/in.2009.9.6.265 摘要:Bae JY, Moon SH, Choi JA, Park JS, Hahn BS, Kim KY, Kim B, Song JY, Kwon DH, Lee SC, Kim JB, Yang JS. Recombinant DNA and Protein Vaccines for Foot-and-mouth Disease Induce Humoral and Cellular Immune Responses in Mice. Immune Netw. 2009 Dec;9(6):265–73.