对羟基苯甲醇置于1,3-双(2,6-二异丙苯基)-2,2-二氟-2,3-二氢-1H-咪唑,Cesium Fluoride体系中,用 甲苯 作为反应溶剂,化学反应 20.5H,以5%的收率获得产物对氟苯甲醇 参考文献:Deoxyfluorination Of Phenols 标题:Deoxyfluorination Of Phenols 摘要:An Operationally Simple Ipso Fluorination Of Phenols With A New Deoxyfluorination Reagent Is Presented. DOI:10.1021/ja2048072
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-9802952-B2 优先权日:2013-07-15 标 题:Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives 发明人:KOPETZKI DANIEL; MCQUADE DAVID TYLER; SEEBERGER PETER H; GILMORE KERRY 权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V; MAX-PLANK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V 摘要:The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C 1 -C 5 alcohol.
专利号:US-4273947-A 优先权日:1979-01-31 标 题:Hydrogenation of fluorine-containing carboxylic acids 发明人:NOVOTNY MIROSLAV 权利人:ALLIED CHEM 摘要:A process is described for the heterogeneous hydrogenation of fluorine-containing alkyl, cycloalkyl, and benzene carboxylic acids to the corresponding primary alcohols. The hydrogenation can be carried out in the liquid or vapor phase in the presence of a solid rhodium or iridium catalyst, employed as the metal, metallic oxide, or mixture thereof. In the liquid phase, the hydrogenation can be carried out batchwise under mild conditions of temperature and pressure, preferably at about 50°-150° C. and about 5-15 atmospheres, in an atmosphere containing hydrogen gas. A preferred embodiment is the hydrogenation of trifluoroacetic acid in the liquid phase to 2,2,2-trifluoroethanol, said alcohol being useful as an intermediate in the synthesis of the anesthetic, isoflurane, CF 3 CHClOCHF 2 .
专利号:US-9334230-B2 优先权日:2009-09-18 标题:Process of forming an amide 发明人:HONG SOON HYEOK; GHOSH SUBHASH CHANDRA; ZHANG YAO; MUTHAIAH SENTHILKUMAR; CHEN CHENG; XU XIANGYA 权利人:HONG SOON HYEOK; GHOSH SUBHASH CHANDRA; ZHANG YAO; MUTHAIAH SENTHILKUMAR; CHEN CHENG; XU XIANGYA; UNIV NANYANG TECH 摘要:A process is provided for the synthesis of an amide. A primary or secondary amine and a primary alcohol, with the amine and the alcohol being either moieties of different reactants or moieties of the same molecule, are contacted in the presence of a Ruthenium (II) catalyst. The Ruthenium (II) catalyst is free of a phosphine ligand. The process is also carried out in the absence of a phosphine. Providing the Ruthenium (II) catalyst includes providing an N-heterocyclic carbene.
专利号:US-7148362-B2 优先权日:2003-09-18 标题:Process for the preparation of enantiopure pyrrolidin-2-one derivatives 发明人:IDING HANS; KRUMMENACHER DANIELA; WIRZ BEAT; WOSTL WOLFGANG 权利人:HOFFMANN LA ROCHE 摘要:The present invention relates to a process for the preparation of enantiopure intermediates useful in the synthesis of valuable pharmaceutically active compounds, e.g. MAOB inhibitors, and to novel intermediates of formulae I and II n nwherein R 21 , R 22 , R 23 and R 24 are as defined in the description and claims.
专利号:US-12145139-B2 优先权日:2016-02-09 标题 :Manganese based complexes and uses thereof for homogeneous catalysis 发明人:MILSTEIN DAVID; NERUSH ALEX; VOGT MATTHIAS; MUKHERJEE ARUP; ESPINOSA-JALAPA NOEL ANGEL; CHAKRABORTY SUBRATA 权利人:YEDA RES & DEV; NERUSH ARKADI 摘要:The present invention relates to novel manganese complexes and their use, inter alia, for homogeneous catalysis in (1) the preparation of imine by dehydrogenative coupling of an alcohol and amine; (2) C—C coupling in Michael addition reaction using nitriles as Michael donors; (3) dehydrogenative coupling of alcohols to give esters and hydrogen gas (4) hydrogenation of esters to form alcohols (including hydrogenation of cyclic esters (lactones) or cyclic di-esters (di-lactones), or polyesters); (5) hydrogenation of amides (including cyclic dipeptides, lactams, diamide, polypeptides and polyamides) to alcohols and amines (or diamine); (6) hydrogenation of organic carbonates (including polycarbonates) to alcohols or hydrogenation of carbamates (including polycarbamates) or urea derivatives to alcohols and amines; (7) dehydrogenation of secondary alcohols to ketones; (8) amidation of esters (i.e., synthesis of amides from esters and amines); (9) acylation of alcohols using esters; (10) coupling of alcohols with water and a base to form carboxylic acids; and (11) preparation of amino acids or their salts by coupling of amino alcohols with water and a base. (12) preparation of amides (including formamides, cyclic dipeptides, diamide, lactams, polypeptides and polyamides) by dehydrogenative coupling of alcohols and amines; (13) preparation of imides from diols.
摘要:Campagne, J. M.; Leclerc, E., Science of Synthesis Knowledge Updates, (2020) 2, 188. 摘要:Braun, M., Science of Synthesis Knowledge Updates, (2017) 1, 465. 摘要:Vashchenko, B. V.; Grygorenko, O. O., Science of Synthesis Knowledge Updates, (2021) 3, 410. 摘要:Scammells, P. J., Science of Synthesis Knowledge Updates, (2013) 2, 445. 摘要:Scammells, P. J., Science of Synthesis Knowledge Updates, (2013) 2, 454.