1,3-Dioxo-1-(Phenylamino)Butan-2-Yl Acetate置于potassium Carbonate,对甲苯磺酸体系中,用 甲苯 作为反应溶剂,化学反应 49.17H,反应生成 萎锈灵 参考文献:Synthesis Of Sulfur-Oxygen-Transposed Dihydro-1,4-Oxathiin Derivative By Unusual Rearrangement Of .Beta.-Hydroxy-1,3-Oxathiolanes 标题:Synthesis Of Sulfur-Oxygen-Transposed Dihydro-1,4-Oxathiin Derivative By Unusual Rearrangement Of .Beta.-Hydroxy-1,3-Oxathiolanes 摘要: DOI:10.1021/jo00271A043
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).
专利号:US-2024383940-A1 优先权日:2021-03-31 标题 :Synthesis of trinucleotide and tetranucleotide caps for mrna production 发明人:ENDO ATSUSHI 权利人:MODERNA TX INC 摘要:Provided herein are methods of making trinucleotides and tetranucleotides for use as 5′ mRNA caps. The methods utilize a novel “top-down†strategy and provide for synthesis of oligonucleotides with higher yields and increased efficiency compared to traditional methods. A key step of the methods disclosed, herein can also be adapted to utilize a “one-pot†approach, resulting in an increase in the yield of the final oligonucleotide product.
专利号:US-11518780-B2 优先权日:2019-07-31 标 题:Sensitive oligonucleotide synthesis using sulfur-based functions as protecting groups and linkers 发明人:FANG SHIYUE 权利人:FANG SHIYUE 摘要:Embodiments for the synthesis of sensitive oligonucleotides as well as insensitive oligonucleotides are provided. Sulfur-based groups are used for the protection of exo-amino groups of nucleobases, phosphate groups and 2′—OH groups, and as cleavable linker for linking oligonucleotides to a support. Oligonucleotide syntheses are achieved under typical conditions using phosphoramidite chemistry with important modifications. To prevent replacing sulfur-based protecting groups by acyl groups via cap-exchange, special capping agents are used. To retain hydrophobic tag to assist RP HPLC purification, special phosphoramidites are used in the last synthetic cycle. With the sulfur-based groups for protection and linking, oligonucleotide deprotection and cleavage are achieved via oxidation followed by beta-elimination under mild conditions. Therefore, besides for insensitive oligonucleotide synthesis, the embodiments of the invention are capable for the synthesis of oligonucleotide analogs containing sensitive functional groups that cannot survive the harsh conditions used in prior art oligonucleotide synthesis technologies.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2023357286-A1 优先权日:2020-07-24 标 题:Ketone synthesis and applications 发明人:KISHI YOSHITO; UMEHARA ATSUSHI 权利人:HARVARD COLLEGE 摘要:Provided are new nickel./zirconium-mediated coupling reactions useful in the synthesis of ketone-containing compounds, e.g., halichondrin natural products and related molecules. A feature of the present disclosure is the use of a nickel(I) catalyst in tandem with a nickel (II) catalyst in the Ni/Zr-mediated coupling reactions. Without wishing to be bound by any particular theory, the nickel (I) catalyst selectively activates the electrophilic coupling partner (i.e., the compound of Formula (A)), and the nickel(ll) catalyst selectively activates the nucleophilic coupling partner (i.e., a thioester of Formula (B)). This dual catalyst system leads to improved coupling efficiency and eliminates the need for a large excess of one of the coupling partners (i.e., a compound of Formula (A) or (B)).
1: Shima Y, Ito Y, Hatabayashi H, Koma A, Yabe K. Five carboxin-resistant mutants exhibited various responses to carboxin and related fungicides. Biosci Biotechnol Biochem. 2011;75(1):181-4. Epub 2011 Jan 7. 3: Ngari C, Combier JP, Doré J, Marmeisse R, Gay G, Melayah D. The dominant Hc.Sdh (R) carboxin-resistance gene of the ectomycorrhizal fungus Hebeloma cylindrosporum as a selectable marker for transformation. Curr Genet. 2009 Apr;55(2):223-31. doi: 10.1007/s00294-009-0231-4. Epub 2009 Feb 13. doi: 10.1186/s13568-016-0232-x. Epub 2016 Aug 24. 6: Kilaru S, Collins CM, Hartley AJ, Burns C, Foster GD, Bailey AM. Investigating dominant selection markers for Coprinopsis cinerea: a carboxin resistance system and re-evaluation of hygromycin and phleomycin resistance vectors. Curr Genet. 2009 Oct;55(5):543-50. doi: 10.1007/s00294-009-0266-6. Epub 2009 Jul 28. Russian. doi: 10.1094/PHYTO.2000.90.2.179. doi: 10.1111/1462-2920.12282. Epub 2013 Oct 10. doi: 10.1016/j.fgb.2008.10.005. Epub 2008 Oct 21.
合成参考文献
摘要:Archives of Environmental Contamination and Toxicology., 12(355), 1983 [] 摘要:Gosselin, R.E., R.P. Smith, H.C. Hodge. Clinical Toxicology of Commercial Products. 5th ed. Baltimore: Williams and Wilkins, 1984., p. II-317 摘要:USEPA/Office of Water; Federal-State Toxicology and Risk Analysis Committee (FSTRAC). Summary of State and Federal Drinking Water Standards and Guidelines (11/93) To Present 摘要:Menzie, C.M. Metabolism of Pesticides-Update III. Special Scientific Report- Wildlife No. 232. Washington, DC: U.S.Department of the Interior, Fish and Wildlife Service, 1980., p. 113 摘要:USEPA/Office of Pesticide Programs; Reregistration Eligibility Decision Document - Carboxin. EPA 738-R-04-015 September 2004. Available from, as of April 22, 2005: https://cfpub.epa.gov/oppref/rereg