专利号:US-12410140-B2 优先权日:2020-06-19 标题:Method for synthesis of roxadustat and intermediate thereof, and intermediate thereof 发明人:ZHANG YONG; WANG GUO; YANG FEI; LIU FENGWEI; ZHOU CHUNDONG; ZHANG ZITONG 权利人:JUMPCAN SHANGHAI MEDICAL TECH CO LTD 摘要:Disclosed are a method for the synthesis of roxadustat and an intermediate thereof, and an intermediate thereof. In particular, disclosed is a method for the synthesis of compound M1, the method comprising the following steps: carrying out a reaction as shown below between compound SM and compound SM-A under the action of an oxidizing agent. The method of the present invention uses cheap and easily available raw materials, has short reaction steps, produces a high yield, has simple and convenient post-treatment procedures, and is suitable for industrial production.
专利号:US-7276637-B2 优先权日:2002-08-02 标题:Synthesis of cyclohexanone derivatives 发明人:BRANDS KAREL MARIE JOSEPH; DAVIES ANTONY JOHN; OAKLEY PAUL JOSEPH; SCOTT JEREMY PETER; SHAW DUNCAN EDWARD; TEALL MARTIN RICHARD 权利人:MERCK & CO INC 摘要:A novel process for preparing cyclohexanone derivatives of formula (I) n nis described. The products are useful as gamma secretase inhibitors, or as intermediates in the synthesis of other gamma secretase inhibitors.
专利号:US-8729308-B2 优先权日:2009-12-01 标 题:Process for the preparation of tapentadol and intermediates thereof 发明人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO 权利人:MOTTA GIUSEPPE; VERGANI DOMENICO; BERTOLINI GIORGIO; EUTICALS SPA 摘要:The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below n nusing the (2R,3R)—O,O′-dibenzoyltartaric chiral acid wherein said resolution is quantitative.n n The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.
专利号:WO-2014202765-A1 优先权日:2013-06-21 标题 :Preparation of chiral 1-methyl-2,3,4,5-1h-benzodiazepines via asymmetric reduction of alpha-substituted styrenes 发明人:STAVBER GAJ; GAZIC SMILOVIC IVANA; CLUZEAU JEROME; RICHTER FRANK 权利人:LEK PHARMACEUTICALS 摘要:The present invention provides an asymmetric and economic synthesis of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1 H-benzo[d]azepine via novel intermediates applying an asymmetric enzymatic, biomimetic or catalytic reduction. The present invention also provides a novel green asymmetric catalytic reduction adapted for an aqueous medium to be applied in the synthesis of 8-chloro-1-methyl-2,3,4,5-tetrahydro-1 H-benzo[d]azepine or novel intermediates.
专利号:US-6110907-A 优先权日:1997-04-30 标题 :Synthesis of platinum complexes and uses thereof 发明人:AU-YEUNG STEVE C F; HO YEE PING; GE LIN; XIUWEN HAN; XINNING WANG; SHIWEI LU; TAO JIANG 权利人:DALIAN CHEMICAL PHYSICS INST; UNIV HONG KONG CHINESE 摘要:This invention provides novel antitumor demethylcantharidin platinum complexes. This invention also provides a composition comprising at least one of said demethylcantharidin platinum complexes and a suitable carrier. This invention provides a pharmaceutical composition comprising effective amount of at least one of the said demethylcantharidin platinum complexes and a pharmaceutically acceptable carrier. This invention provides a method of inhibiting the growth of tumorous cells comprising contacting the cells with an amount of said demethylcantharidin platinum complex effective to inhibit the growth of said tumorous cells. This invention provides a method of inhibiting the growth of tumorous cells in a subject comprising administering to the subject with an amount of the said demethylcantharidin platinum complexes effective to inhibit the growth of said tumorous cells in the subject. Finally, this invention provides methods for producing said demethylcantharidin platinum complexes.
专利号:US-5760262-A 优先权日:1996-09-17 标题 :Enhanced production of bridged hafnocenes 发明人:DESOTO TROY E; LIN RONNY W; BALHOFF JOHN F 权利人:ALBEMARLE CORP 摘要:The reaction between a hafnium tetrahalide-diamine adduct and a metallated bis(cyclopentadienyl-moiety containing) ligand, offers great promise as a way of producing racemic hafnocenes, but involves a number of complications. Tetrahydrofuran, a commonly-used solvent/diluent for such reactions, when present in substantial portions in the liquid reaction medium containing the reactants and/or reaction product(s) has been found to cause a substantial reduction in yields of chiral hafnocenes. Apparently the presence of a substantial amount of THF causes or at least results in the formation of increased amounts of the undesirable meso isomer, tends to cause or result in tar formation, and results in a product having poor filterability. Thus large amounts of THF if fed to the reactor with the reactant(s) are purged to a suitably low level, replaced by a liquid aromatic hydrocarbon, and then the reaction mixture is heated to a higher reaction temperature. Large amounts of liquid paraffins and free diamine in the reaction mixture during reaction also contribute to tar formation and reduction in yields of chiral hafnocene. Thus the presence of such materials in the reaction mixture is kept to a minimum. These process modifications make it possible to increase yields of the chiral hafnocene, to reduce formation of the meso isomer, and to sharply reduce the amount of tar formation in the synthesis of chiral hafnocenes from diamine adducts of hafnium tetrahalide and metallated bis(cyclopentadienyl-moiety containing) ligands. Moreover, the hafnocene reaction product so formed has significantly improved filterability characteristics.