专利号:US-2024308959-A1 优先权日:2021-06-29 标 题:Processes for the preparation of (s)-2-(4-chloro-2-methoxyphenyl)-2-((3 -methoxy-5-(m ethylsulfonyl)phenyl)amino)-1 -(1h-indol-3-yl)ethenone derivatives 发明人:WU KAI; OOST RIK; SCHWEITZER-CHAPUT BERTRAND; ERIKSSON CARL ARNE MAGNUS; COESEMANS ERWIN 权利人:JANSSEN PHARMACEUTICALS INC 摘要:The present invention relates to novel chiral synthesis of mono- or di-substituted indole compounds of formula (I) n n n n n n n n n n n n wherein: n R 1 is H, R 2 is F and R 3 is H or CH 3 , n R 1 is H, CH 3 or F, R 2 is OCH 3 and R 3 is H and n R 1 is H, R 2 is OCH 3 and R 3 is CH 3 , n R 1 is CH 3 , R 2 is F and R 3 is H, n R 1 is CF 3 or OCF 3 , R 2 is H and R 3 is H, n R 1 is OCF 3 , R 2 is OCH 3 and R 3 is H and n R 1 is OCF 3 , R 2 is H and R 3 is CH 3 .
专利号:US-2025256963-A1 优先权日:2024-02-12 标题:Synthesis of nano-hydroxyapatite from decarbonized eggshells 发明人:AHMED MORSI MOHAMED MAHMOUD MORSI 权利人:UNIV KING FAHD PET & MINERALS 摘要:A method of synthesizing a hydroxyapatite (HAp) product from eggshells, including reacting eggshells with an inorganic base in a polar solvent to decarbonize the eggshells and form a calcium hydroxide material and a sodium carbonate material and mixing the calcium hydroxide material, in a polar solvent at a pH of greater than 10, with a phosphate salt to form a mixture including the hydroxyapatite product. A ratio of the calcium hydroxide material to the phosphate salt is from 1:1 to 5:1. The method further includes microwave irradiating the mixture for 1 to 10 minutes (min) at a temperature from 80 to 120 degrees Celsius (° C.), filtering the mixture to collect the hydroxyapatite product, and further drying the hydroxyapatite product.
专利号:WO-2004009574-A1 优先权日:2002-07-22 标 题 :Synthesis of discodermolide 发明人:FLORENCE GORDON; KOCH GUIDO; LOISELEUR OLIVIER; MICKEL STUART JOHN; PATERSON IAN 权利人:NOVARTIS AG; NOVARTIS PHARMA GMBH; UNIV CAMBRIDGE TECH; FLORENCE GORDON; KOCH GUIDO; LOISELEUR OLIVIER; MICKEL STUART JOHN; PATERSON IAN 摘要:The invention relates to a process for preparing discodermolide, for preparing intermediates for the manufacture of discodermolide and discodermolide analogues and to the intermediates obtained during the process. Wherein the process proceeds via a tetraene of formula (IV).
专利号:US-6989401-B2 优先权日:2000-07-19 标题:Sulfonic acid derivatives of hydroxamic acids and their use as medicinal products 发明人:MAEDA KAZUHIRO; SONDA SHUJI; TAKEMOTO TADAHIRO; GOTO TOMOKAZU; KOBAYASHI FUJIO; KAJII MASAHIKO; KOMORITA NARUYASU; HIRAYAMA FUMIHIRO 权利人:MITSUBISHI PHARMA CORP 摘要:The present invention relates to a novel sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof. More particularly, the present invention relates to a sulfonic acid derivative of hydroxamic acid or a pharmacologically acceptable salt thereof, which is useful as an inhibitor of lipopolysaccharides (LPS). In addition, the present invention relates to a novel intermediate compound useful for the synthesis of this sulfonic acid derivative of hydroxamic acid.
专利号:US-8884001-B2 优先权日:2008-05-08 标题:Preparation of intermediates useful in the synthesis of 2′-cyano-2′-deoxy-N4-palmi-toyl-1-β-D-arabinofuranosylcytosine 发明人:WOOD GAVIN; WESTWOOD ROBERT; Murofushi tsuyoshi; NUMAGAMI EIJI; TAKITA TAKASHI 权利人:WOOD GAVIN; WESTWOOD ROBERT; Murofushi tsuyoshi; NUMAGAMI EIJI; TAKITA TAKASHI; CYCLACEL LTD 摘要:The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2′ into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2′-cyano-2′-deoxy-N 4 -palmitoyl-1-β-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
专利号:WO-2022127321-A1 优先权日:2020-12-18 标题 :Novel intermediate, preparation method for same, and applications thereof 发明人:QIN YONG; ZHONG WU; LI SONG; XUE FEI; SONG HAO; LIU XIAOYU; ZHANG DAN; HE HUAN; Xue Fanglin; ZHANG MAOJIE; HU ZHAO; LI CHUNXIN; ZHU JIANQUAN; ZHANG YIFAN; TANG YU; WANG RUI; LI XUE; CAI YUKUN 权利人:UNIV SICHUAN 摘要:The invention relates to the field of medicament synthesis and specifically to a novel intermediate, a preparation method for same, and applications thereof. The structural formula of the novel intermediate of the present application is as represented by formula (I): in which R is a secondary amine protecting group. The present invention, based on possible biogenetic pathways of morphine derivatives, by means of a strategy for biomimetic synthesis, with an asymmetric transfer hydrogenation reaction and an intramolecular oxidative dearomatization Heck reaction in the preparation process of the intermediate serving as key reactions for total synthesis, implements the highly efficient synthesis of the morphine derivatives. The synthesis of the morphine derivatives starting from the novel intermediate provided in the present invention is characterized by significantly reduced synthesis steps, an increased yield, a reduced discharge of gaseous, liquid, and solid wastes, and inexpensive production costs.
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