专利号:US-8779207-B2 优先权日:2012-08-31 标题 :Method for synthesis of [6,6]-phenyl-C61-butyric acid methyl ester (PCBM) and fullerene derivatives 发明人:NG KA MING; ZHUANG JIANLE; TSENG NAI WEN; YU YONG 权利人:NG KA MING; ZHUANG JIANLE; TSENG NAI WEN; YU YONG; NANO & ADVANCED MATERIALS INST LTD 摘要:The present subject matter relates to methods for the synthesis of [6,6]-phenyl-C 61 -butyric acid methyl ester (PCBM) and fullerene derivatives in a yield of at least 40%.
专利号:US-5089647-A 优先权日:1989-03-09 标题:Method for preparing intermediates for the synthesis of steroid side chains in optically active form 发明人:DELUCA HECTOR F; SCHNOES HEINRICH K; PERLMAN KATO L 权利人:WISCONSIN ALUMNI RES FOUND 摘要:This invention provides a novel method for the preparation of optically active arylalykylsulfone derivatives, having a chiral center in the alkyl moiety in either the (R)- or the (S)-configuration. These optically active sulfones find use in the stereospecific synthesis of steroid or vitamin D compounds having chiral center at either carbon 24 or carbon 25 of the side chain. The method comprises the steps of reacting an optically active sulfinate ester having a chiral center at sulfur with a racemic alkyl Grignard reagent to obtain a mixture of diastereomeric sulfoxides, separating the mixture of diastereomeric sulfoxides, and oxidizing separately each of the diastereomers to obtain the desired optically active sulfone.
专利号:US-11008285-B2 优先权日:2017-03-27 标 题 :Process for synthesis of mesotrione 发明人:GHARDA KEKI HORMUSJI; MATHUR SUCHET SARAN; JAIN NANDKUMAR JANARDAN; SATHE SHEKHAR VISHWANATH; DAMANIA PRAGNESH DALPATRAM 权利人:GHARDA CHEMICALS LTD 摘要:The present disclosure relates to a process for synthesis of mesotrione. The process comprises reacting 4-toluene sulfonyl chloride with alkali metal sulphite and alkali metal bicarbonate to obtain alkali metal toluene-4-sulfinate. The alkali metal toluene-4-sulfinate is reacted with alkali metal salt of monochloroacetic acid to obtain 4-methylsulfonyl toluene. Further, 4-methylsulfonyl toluene is nitrated to obtain 2-nitro-4-methylsulfonyl toluene. 2-nitro-4-methylsulfonyl toluene is oxidized and then halogenated to obtain 2-nitro-4-methylsulfonylbenzoyl halide. 2-nitro-4-methylsulfonylbenzoyl halide is reacted with alkali metal salt of 1,3-cyclohexanedione to obtain 3-(2-Nitro-4-methylsulfonylbenzoyloxy)cyclohexen-1-one which is reacted with base, a third fluid medium and cyanide ion source to obtain an amorphous mesotrione. The present disclosure also discloses the steps of converting the amorphous mesotrione to crystalline mesotrione having purity greater than 99%. The process of the present disclosure for preparing mesotrione is rapid, economic, and environment friendly.
专利号:US-9650330-B2 优先权日:2013-12-12 标题 :Process for the synthesis of aryl sulfones 发明人:MHASKE SANTOSH BABURAO; PANDYA VIRAT 权利人:COUNCIL SCIENT IND RES 摘要:The present patent discloses a novel, efficient and transition-metal-free room temperature single step process for synthesis of aryl sulfones and substituted aryl sulfones starting from aryl substrates.
专利号:US-5631384-A 优先权日:1992-09-22 标 题:Areno [e]indols, preparation method and application as intermediates in the synthesis of products with antitumoral activity 发明人:ALEXANDER KOEN; DELAMANO GARCIA JOSE; SAS BENEDIKT; TOJO SUAREZ GABRIEL; GARCIA GRAVALOS DOLORES 权利人:PHARMA MAR S A PHARMAR 摘要:The compounds (I) are useful as intermediates in the synthesis of hexahydroareno(e)cyclopropa(c)indol-4-ones with antitumoral activity.
专利号:US-10905769-B2 优先权日:2015-11-13 标 题:Peptide and peptide mimetic binding antagonists of polo-like kinase 1 polo box domain and methods of use 发明人:BURKE JR TERRENCE R; HYMEL DAVID T; TSUJI KOHEI 权利人:THE US SECRETARY DEPARTMENT OF HEALTH & HUMAN SERVICES 摘要:The description provides novel compounds that may serve as anticancer therapeutics. The compounds of the description bind to polo-like kinases through the polo-box domain. The peptide derivatives of the description have achieved improved efficacy in biochemical assays against Plk1. Exemplary compounds of the description include macrocyclic peptidomimetics with high affinity and selectivity for polo-like kinases, which may provide the basis for a new genre of anticancer therapeutics. Other exemplary compounds of the description include bi-valent compounds with that bind to polo-like kinases through both kinase domain and polo-box domain simultaneously by incorporating additional moieties that target Plk1 kinase domain, which significantly enhances affinitity relative and may provide the basis for a new genre of anticancer therapeutics. The description also provides methods of use, methods of preparation, compositions, and kits thereof. Further, the description provides a novel method of design and/or synthesis of phosphoryl-derived peptide derivatives useful as therapeutic agents.
摘要:Silva, V. L. M.; Pinto, D. C. G. A.; Santos, C. M. M.; Rocha, D. H. A., Science of Synthesis Knowledge Updates, (2022) 3, 322. 摘要:Kawęcki, R., Science of Synthesis Knowledge Updates, (2018) 4, 290. 摘要:Haufe, G., Science of Synthesis Knowledge Updates, (2019) 3, 240. 摘要:Zhang, M.; Su, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 131. 摘要:Ruffoni, A.; Leonori, D., Science of Synthesis: Photocatalysis in Organic Synthesis, (2018) 1, 548.