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-9695188-B2 优先权日:2013-12-06 标 题 :Methods useful in the synthesis of halichondrin B analogs 发明人:HU YONGBO; ZHANG HUIMING; CHIBA HIROYUKI; KOMATSU YUKI; LEWIS BRYAN M 权利人:EISAI R&D MAN CO LTD 摘要:In general, the present invention features improved methods useful for the synthesis of analogs of halichondrin B, such as eribulin and pharmaceutically acceptable salts thereof (e.g., eribulin mesylate).
专利号:US-9802953-B2 优先权日:2007-10-03 标 题 :Intermediates and methods for the synthesis of halichondrin B analogs 发明人:CHASE CHARLES E; ENDO ATSUSHI; FANG FRANCIS G; LI JING 权利人:EISAI R&D MAN CO LTD 摘要:Methods of synthesizing intermediates useful for the synthesis of halichondrin B analogs are described.
专利号:US-6255092-B1 优先权日:1993-09-24 标题:Stereospecific alcohol dehydrogenase isolated from Candida parapsilosis, amino acid and DNA sequences therefor, and method of preparation thereof 发明人:KOJIMA TOMOKO; YAMAMOTO HIROAKI; KAWADA NAOKI; MATSUYAMA AKINOBU 权利人:DAICEL CHEM 摘要:The present invention provides a novel secondary alcohol dehydrogenase useful for the synthesis of optically active alcohol and DNA encoding said enzyme. A microorganism belonging to genus Candida was found to produce a novel secondary alcohol dehydrogenase with a high stereochemical specificity. Using said enzyme, optically active alcohols were prepared, and by cloning of DNA encoding said enzyme, the base sequence of said DNA was determined. By providing a novel secondary alcohol dehydrogenase with a high stereochemical specificity and the gene encoding said enzyme, an efficient production of optically active alcohols became possible.
专利号:WO-9931506-A9 优先权日:1997-12-18 标题:Parallel solution phase synthesis of lactams 发明人:CWI CYNTHIA LYNN; SCOTT WILLIAM LEONARD 权利人:LILLY CO ELI; CWI CYNTHIA LYNN; SCOTT WILLIAM LEONARD 摘要:The present invention provides a parallel solution phase process for making combinatorial arrays of lactam derivatives which are useful for screening for therapeutically useful compounds.
专利号:US-2021379557-A1 优先权日:2018-10-23 标题 :A system and method for promoting chemical reactions 发明人:NAAMAN RON; FONTANESI CLAUDIO; TASSINARI FRANCESCO; MISHRA SURYAKANT; CAPUA EYAL; PALTIEL YOSSEF; YOCHELIS SHIRA; METZGER TZURIEL 权利人:YEDA RES & DEV; YISSUM RES DEV CO OF HEBREW UNIV JERUSALEM LTD 摘要:A system and method for use in synthesis and promoting interactions of chiral molecules. The system can include: a container configured for containing fluid mixture comprising one or more reactant molecules and at least one surface comprising ferromagnetic or paramagnetic material located to be in at least partial contact with reactants in said container. The ferromagnetic of paramagnetic material can be magnetizable with magnetization direction perpendicular to said at least one surface, thereby providing chiral selective synthesis from said one or more reactant molecules. The technique can enable selective interactions of enantiomers of selected handedness of chiral molecules or formation of selected enantiomers from achiral molecule reactants.
摘要:Schmidberger, J. W.; Hepworth, L. J.; Green, A. P.; Flitsch, S. L., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 335. 摘要:Rodríguez-Mata, M.; Gotor-Fernández, V., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 206. 摘要:HANSCH,C ET AL. (1995) 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Wang, L.; Liu, M.; Cheng, J., Science of Synthesis: Knowledge Updates, (2024) 1, 183.