专利号:US-6350878-B1 优先权日:1998-05-18 标 题 :Intermediates for the synthesis of epothilones and methods for their preparation 发明人:ALTMANN KARL-HEINZ; BAUER ARMIN; SCHINZER DIETER 权利人:NOVARTIS AG 摘要:The invention relates to a method of synthesis for a compound of formula (I),wherein R is a heterocyclyl moiety and X1, X2, X3 and X4 are, independently of each other, protecting groups, which is appropriate for the synthesis of epothilone B and desoxyepothione B.
专利号:US-9809566-B2 优先权日:2012-09-06 标题:Organocatalytic process for asymmetric synthesis of decanolides 发明人:RAWAT VARUN; DEY SOUMEN; SHELKE ANIL MARUTI; SURYAVANSHI GURUNATH MALLAPPA; SUDALAI ARUMUGAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses organocatalytic process for asymmetric synthesis of highly enantioselective decanolide compounds in high yield with >99% ee. Further, the present invention disclose cost effective, improved organocatalytic process for asymmetric synthesis of highly enantioselective decanolides compounds from non-chiral, cheap, easily available raw materials.
专利号:US-4190579-A 优先权日:1977-12-29 标题:Synthesis of beta-lactams from azetidine carboxylic acid esters 发明人:LIPSHUTZ BRUCE H; WASSERMAN HARRY H; WU JAMES S 权利人:RESEARCH CORP 摘要:Azetidine carboxylic acid esters are converted into enol silyl ethers which, as enamino ketene acetals, undergo ready oxidative cleavage of the ethylenically unsaturated double bond, e.g. by dye-sensitized photo-oxygenation, to form beta-lactams. The beta-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams.
专利号:US-11524957-B2 优先权日:2018-04-02 标 题 :Process for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one 发明人:ZHU LEI; BAILEY JOHN DANIEL; DURAK LANDON; WAETZIG JOSHUA DAVID; MIZUNO MASAHIRO; MAEDA KAZUHIRO; YASUMA TSUNEO; YAMAGUCHI HIROSHI; FUKUOKA KOICHIRO; AKIYAMA KAZUYUKI 权利人:TAKEDA PHARMACEUTICALS CO 摘要:The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.
专利号:US-12391691-B2 优先权日:2018-11-16 标题:Synthesis of key intermediate of KRAS G12C inhibitor compound 发明人:PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY 权利人:AMGEN INC 摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as
专利号:US-5656662-A 优先权日:1990-01-12 标 题:Synthesis of optically pure 4-alkenyl- or 4-alkanyl-2-hydroxytetronic acids 发明人:MANTRI PADMAJA; WITIAK DONALD T 权利人:UNIV OHIO STATE RES FOUND 摘要:The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, thus making them useful in the treatment of coronary artery diseases, especially atherosclerosis, and additionally, as inhibitors of various inflammatory cytokines, making them useful in the treatment of both acute and chronic inflammation, as well in the treatment of cachexia, rheumatoid arthritis, multiple sclerosis, Crohn's disease and ulcerative colitis. The invention further relates to pharmaceutical compositions of the instant compounds.
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合成参考文献
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