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-10973847-B2 优先权日:2017-06-30 标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof 发明人:JOHNSON JEREMIAH A; GOLDER MATTHEW R 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.
专利号:US-12221452-B2 优先权日:2017-10-04 标题:Synthesis of cantharidin 发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R 权利人:VERRICA PHARMACEUTICALS INC 摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-4284582-A 优先权日:1978-04-28 标 题 :Process for the preparation of cyclopropane derivatives, intermediates in the synthesis of pyrethroid insecticides 发明人:KAYE ALBERT E; TUCKER ALAN C 权利人:ICI LTD 摘要:Compounds of formula: wherein both groups X are chlorine, bromine or trifluoromethyl, or one X is chlorine or bromine and the other is trifluoromethyl, and Y is -CN or -COOR in which R is an alkyl group, are obtained by (A) reacting a compound of the formula: wherein X1 is chlorine or bromine, with a compound of the formula: X2C=CH-CH=C(CH3)2 in the presence of metallic copper or at least one copper salt and a base, or (B) reacting a compound of the formula: Y-CH2-CN with a compound of the formula: X2C=CH-CH=C(CH3)2 and chlorine or bromine, in the presence of at least one reducible copper salt and a base, or (C) reacting a compound of formula: X-CH2-CN with a compound of the formula: wherein X1 is chlorine or bromine, in the presence of at least one copper salt. The compounds are intermediates in the synthesis of pyrethroid insecticides.
专利号:US-9611255-B2 优先权日:2015-06-10 标题 :Process for total synthesis of flavonoid compounds and isomers thereof 发明人:RAO BATCHU VENKATESWARA; LINGAMURTHY MACHA; RAJU Gurrapu; SARMA VANKA UMAMAHESWARA 权利人:COUNCIL SCIENT IND RES; COUNCIL SCIENT IND RES 摘要:The present invention relates to the a process for total synthesis of flavonoid compounds of general formula I and isomers thereof n nwherein R 1 and R 2 is OH; R 3 â• H orn n n n n n n n n n n The present invention particularly relates to the process for preparation and separation of (2S,3S)-taxifolin-6-C-β-D-glucopyranoside (ulmoside A), (2R,3R)-taxifolin-6-C-β-D-glucopyranoside and taxifolin.
专利号:US-11807884-B2 优先权日:2017-12-09 标题:Generation-dependent supramolecular assemblies of protein-dendron conjugates 发明人:BRITTO Sandanaraj Selvaraj; BHANDARI PAVANKUMAR JANARDHAN; REDDY Mullapudi Mohan 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES 摘要:The present invention discloses monodisperse protein-dendron conjugates that self-assemble to generation-dependent supramolecular protein assemblies of different size and surface charges. The invention further provides a process for synthesis of protein-dendron conjugates containing hydrophobic dendron of different generations.
摘要:Journal of Industrial Hygiene and Toxicology., 23(259), 1941 摘要:Archiv fuer Gewerbepathologie und Gewerbehygiene., 5(1), 1933 摘要:IPCS, CEC; International Chemical Safety Card on 2-Methoxyethyl acetate (November 2003). Available from, as of March, 15 2009: 摘要:Bridie AL et al; Water Res 13 (7): 623-6 (1979) Available from, as of January 20, 2009 摘要:NIOSH; NOES. National Occupational Exposure Survey conducted from 1981-1983. Estimated numbers of employees potentially exposed to specific agents by 2-digit standard industrial classification (SIC). Available at https://www.cdc.gov/noes/ as of Feb 2, 2009.