专利号:US-5338851-A 优先权日:1993-03-31 标 题:Synthesis of cis-decahydroisoquinoline-3-carboxylic acids 发明人:HUFF BRET E; KHAU VIEN V; MARTINELLI MICHAEL J; PETERSON BARRY C 权利人:LILLY CO ELI 摘要:This invention provides a process for the synthesis of cis-decahydroisoquinoline-3-carboxylic acids and provides intermediates in the synthesis thereof.
专利号:US-7888337-B2 优先权日:2007-08-31 标 题 :Synthesis of oseltamivir containing phosphonate congeners with anti-influenza activity 发明人:WONG CHI-HUEY; FANG JIM-MIN; SHIE JIUN-JIE; CHENG YIH-SHYUN EDMOND; JAN JIA-TSRONG 权利人:ACADEMIA SINICA 摘要:Novel phosphonate compounds are described. The compounds have activity as neuraminidase inhibitors against wild-type and H274Y mutant of H1N1 and H5N1 viruses. The present disclosure also provides an enantioselective synthetic route to known neuraminidase inhibitors oseltamivir and the anti-flu drug Tamiflu®, as well as novel phosphonate compounds, via D-xylose. Another efficient and flexible synthesis of Tamiflu and the highly potent neuraminidase inhibitor Tamiphosphor was also achieved in 11 steps and >20% overall yields from the readily available fermentation product (1S-cis)-3-bromo-3,5 -cyclohexadiene-1,2-diol. Most of the reaction intermediates were obtained as crystals without tedious purification procedures. The key transformations include an initial regio- and stereoselective bromoamidation of a bromoarene cis-dihydrodiol, as well as the final palladium-catalyzed carbonylation and phosphonylation.
专利号:US-5461156-A 优先权日:1993-03-31 标 题 :Stereocontrolled synthesis of cis-bicyclic compounds 发明人:KHAU VIEN V; MARTINELLI MICHAEL J; PETERSON BARRY C; SULLIVAN KEVIN A 权利人:LILLY CO ELI 摘要:This invention provides a process for the stereocontrolled synthesis of cis-bicyclic compounds, including cis-hexahydro-6-isoquinolones, cis-dihydroisochromanones, cis-dihydrothiochromanones, and cisbicyclo[4.4.0]dec-3-ene-2-ones.
专利号:US-3624188-A 优先权日:1968-10-25 标题 :Hypohalogenation of tetramethyl and tetraethyl methylenediphosphonates and trihydrocarbyl phosphonoacetates 发明人:CURRY JOHN DOWNING 权利人:PROCTER & GAMBLE 摘要:The process of reacting either (1) a tetraalkyl (methyl, ethyl, halomethyl or haloethyl) methylenediphosphonate or (2) a trihydrocarbyl (C2-C4) phosphonoacetate with a hypohalite in an aqueous electrolyte solution (preferably in the presence of an inert, water-immiscible, organic solvent) to produce the corresponding mono- and di-halogenated methylenediphosphonate and phosphonoacetate esters. These esters have utility as intermediates in the synthesis of detergent builders and as extreme pressure additives for lubricant compositions.
专利号:US-5442085-A 优先权日:1992-12-04 标 题:Synthesis of tetraalkyl vinylidene diphosphonate monomer 发明人:ALEXANDRATOS SPIRO D 权利人:UNIV TENNESSEE RES CORP 摘要:A method of making a monomer of tetraalkyl vinylidene-1, 1-diphosphonate. The monomer is manufactured by combining an aqueous secondary amine solution with a formaldehyde and a tetra (alkyl) methylene diphosphonate. The resulting mixture is maintained at a pH above about 6 and refluxed for two hours to enable reaction to produce the monomer of tetraalkyl vinylidene-1, 1-diphosphonate. The product monomer is then purified to produce the final end product.
专利号:WO-2021083438-A1 优先权日:2019-10-30 标 题:Inhibitors of purine nucleoside phosphorylase - synthesis and use thereof for treatment of t-cell acute lymphoblastic leukemia and lymphoma 发明人:SKACEL JAN; JANEBA ZLATKO; MERTLIKOVA KAISEROVA HELENA 权利人:USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR V V I 摘要:The present invention relates to new compounds of general formula I, their synthesis, their pharmaceutically acceptable salts, and their use in treatment of T-cell acute lymphoblastic leukemia and lymphoma.
摘要:Abell, A. D.; Edmonds, M. K., Science of Synthesis, (2009) 46, 40. 摘要:Kimura, T., Science of Synthesis Knowledge Updates, (2016) 2, 451. 摘要:Kimura, T., Science of Synthesis Knowledge Updates, (2016) 2, 449. 摘要:Croft, R. A.; Bull, J. A., Science of Synthesis Knowledge Updates, (2018) 4, 413. 摘要:U.S. Army Armament Research & Development Command, Chemical Systems Laboratory, NIOSH Exchange Chemicals., NX#03139