专利号:WO-2021260722-A1 优先权日:2020-06-21 标 题:Design, synthesis of novel oxyindole inhibitors of denv rna dependent rna polymerase 发明人:GUNDLA RAMBABU; ASTHANA SHAILENDRA; BHATTACHARYYA SANKAR; MADDIPATI VENKATANARAYANA CHOWDARY; MITTAL LOVIKA; KAUR JASKARAN; RAWAT YOGITA 权利人:TRANSLATIONAL HEALTH SCIENCE AND TECH INSTITUTE; GANDHI INSTITUTE OF TECH AND MANAGEMENT 摘要:The present invention is drawn to novel compounds of formula I, II and III, including any conformational isomeric form, salts and solvates for inhibition of DENV RNA dependent and RNA polymerase. The present invention also discloses a process of synthesis of the compounds, compositions comprising the said compounds and use of the compounds and treatment comprising the compounds of the present invention.
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-2023312617-A1 优先权日:2020-07-25 标题 :Process for synthesis of organosilicon compounds from halosilanes 发明人:DOLAI SUKANTA; BHAT SHREEDHAR; TARAFDAR GOURAV 权利人:MOMENTIVE PERFORMANCE MAT INC 摘要:A process for synthesis of an organosilicon compound is provided herein. Also, novel organosilicon compounds prepared by the present process is provided herein. The process comprises the reaction of a halosilane with an organofunctional alkyl halide in the presence of a metal catalyst, a promoter, and an optional co-catalyst. The process provides an efficient synthetic route to produce organosilicon compounds. The process also allows synthesis of organosilicon compounds with a plurality of different functional groups.
专利号:US-10053406-B2 优先权日:2015-10-23 标题 :Synthesis of honokiol 发明人:JARACZ STANISLAV; KOZLOWSKI MARISA; EUN LEE YOUNG; KIM SUN MIN 权利人:COLGATE PALMOLIVE CO; UNIV PENNSYLVANIA 摘要:Disclosed herein are improved methods for the synthesis of honokiol, as well as methods for the synthesis of 3,3′-di-tert-butyl-5,5′-dimethyl-[1,1′-biphenyl]-2,4′-diol, 3′,5-dimethyl-[1,1′-biphenyl]-2,4′-diol, and 2,4′-dimethoxy-3′,5-dimethyl-1,1′-biphenyl, 3,3′,5,5′-tetra-tert-butyl-[1,1′-biphenyl]-2,4′-diol, and certain tetrasubstituted bisphenols, and uses therefor.
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-4384127-A 优先权日:1981-04-08 标 题:Process for synthesis of optically pure prostaglandin E2 and analogs thereof 发明人:FUCHS PHILLIP L 权利人:PURDUE RESEARCH FOUNDATION 摘要:The invention comprises a multi-step synthesis of l(-) prostaglandin E 2 . The special features of the synthesis include: (1) a triply-convergent conjugate-addition and alkylation reaction involving the 1,4-addition of a chiral vinyl lithium reagent to a chiral vinylsulfone to produce a sulfone-stabilized anion. This anion is alkylated in situ to produce the basic prostaglandin skeleton structure, which is then subjected to (2) an efficient peracid oxidation of a secondary amine to a β-silyloxy oxime; and (3) an alkali-catalyzed 1,4-elimination of an α-sulfonyl oxime to produce a vinyl nitroso intermediate. This intermediate is treated with borohydride to give a stereospecific 1,4-reduction which yields the bis-silyloxy oxime of l(-)PGE 2 . Hydrolysis of the oxime, with concurrent cleavage of the silyloxy protecting groups, affords l(-)PGE 2 .
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