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-8153839-B2 优先权日:2005-09-14 标题:Method for synthesis of keto acids or amino acids by hydration of acetylene compound 发明人:OGO SEIJI; FUKUZUMI SHUN-ICHI 权利人:OGO SEIJI; FUKUZUMI SHUN-ICHI; JAPAN SCIENCE & TECH AGENCY 摘要:An object of the present invention is to provide a method for synthesis of keto acids by hydration of an acetylene compound (acetylene-carboxylic acids) under mild conditions free from harmful mercury catalysts and a method for synthesis of amino acids from acetylene-carboxylic acids in a single container (one-pot or tandem synthesis). In one embodiment of the method according to the present invention for synthesis of keto acids, acetylene-carboxylic acids is hydrated in the presence of a metal salt represented by General Formula (1), n nwhere M 1 represents an element in Group VIII, IX, or X of the periodic table, and X 1 , X 2 , or X 3 ligand represents halogen, H 2 O, or a solvent molecule, and k represents a valence of a cation species, and Y represents an anion species, and L represents a valence of the anion species, and each of K and L independently represents 1 or 2, and k×m=L×n.
专利号:US-11136335-B2 优先权日:2016-06-30 标题:Prins reaction and intermediates useful in the synthesis of halichondrin macrolides and analogs thereof 发明人:CHASE CHARLES E; CHOI HYEONG-WOOK; ENDO ATSUSHI; FANG FRANCIS G; KIM DAE-SHIK 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of a halichondrin macrolides or analogs thereof through a cyclization reaction strategy. The strategy of the present invention involves subjecting an intermediate to Prins reaction conditions to afford a macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides or analogs thereof and methods for preparing the same.
专利号:US-12146136-B2 优先权日:2020-03-26 标题:Synthesis of modified oligonucleotides with increased stability 发明人:KHVOROVA ANASTASIA; ROUX LOà C MAURICE RENÉ JEAN; YAMADA KEN 权利人:UNIV MASSACHUSETTS 摘要:This disclosure relates to the synthesis of novel modified oligonucleotides. The synthesis of novel phosphoramidites are also provided.
专利号:US-9783549-B2 优先权日:2013-11-04 标题:Macrocyclization reactions and intermediates useful in the synthesis of analogs of halichondrin B 发明人:FANG FRANCIS G; KIM DAE-SHIK; CHOI HYEONG-WOOK; CHASE CHARLES E; LEE JAEMOON 权利人:EISAI R&D MAN CO LTD 摘要:The invention provides methods for the synthesis of eribulin or a pharmaceutically acceptable salt thereof (e.g., eribulin mesylate) through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), Dieckmann reaction, catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic intermediate. The invention also provides compounds useful as intermediates in the synthesis of eribulin or a pharmaceutically acceptable salt thereof and methods for preparing the same.
专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
1: Castro PA, Ramirez A, Sepúlveda FJ, Peters C, Fierro H, Waldron J, Luza S, Fuentealba J, Muñoz FJ, De Ferrari GV, Bush AI, Aguayo LG, Opazo CM. Copper-uptake is critical for the down regulation of synapsin and dynamin induced by neocuproine: modulation of synaptic activity in hippocampal neurons. Front Aging Neurosci. 2014 Dec 3;6:319. doi: 10.3389/fnagi.2014.00319. eCollection 2014. 2: Patel OV, Wilson WB, Qin Z. Production of LPS-induced inflammatory mediators in murine peritoneal macrophages: neocuproine as a broad inhibitor and ATP7A as a selective regulator. Biometals. 2013 Jun;26(3):415-25. doi: 10.1007/s10534-013-9624-4. Epub 2013 Apr 19. doi: 10.1016/j.ejphar.2009.01.008. doi: 10.5740/jaoacint.17-0154. Epub 2017 Sep 15. doi: 10.1021/jacs.7b11372. Epub 2018 Jan 5. doi: 10.1016/bs.mie.2014.11.021. Epub 2015 Jan 14. doi: 10.1016/j.niox.2017.12.003. Epub 2017 Dec 14. doi: 10.1016/j.cbi.2011.03.017. Epub 2011 Apr 8. doi: 10.1007/s10895-016-1930-0. Epub 2016 Sep 19. 13: De Man JG, Moreels TG, De Winter BY, Herman AG, Pelckmans PA. Neocuproine potentiates the activity of the nitrergic neurotransmitter but inhibits that of S-nitrosothiols. Eur J Pharmacol. 1999 Sep 24;381(2-3):151-9. doi: 10.1111/cbdd.12187. Epub 2013 Aug 10.
合成参考文献
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