专利号:US-8809526-B2 优先权日:2010-07-19 标题 :Synthesis of cyclopentaquinazolines 发明人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; DALZIEL SEAN MARK; DAPREMONT Olivier; KIM HYUNJUNG; THOMPSON ANDREW S; ZELLER JAMES ROBERT 权利人:KERSCHEN JAMES ALAN; BRIDGES ALEXANDER JAMES; DALZIEL SEAN MARK; DAPREMONT Olivier; KIM HYUNJUNG; THOMPSON ANDREW S; ZELLER JAMES ROBERT; ONYX PHARMA INC 摘要:A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N—{N-{4-[N-((6S)-2 -hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2 -ynyl)amino]benzoyl}-L-γ-glutamyl}-D-glutamic acid (ONX-0801).
专利号:US-5300638-A 优先权日:1991-07-31 标题:Asymmetric synthesis of taxol side chain 发明人:FARINA VITTORIO; HAUCK SHEILA I 权利人:BRISTOL MYERS SQUIBB CO 摘要:The present invention relates to a process for the preparation of (3R, 4S)-3-hydroxy-4-phenyl-2-azetidinone derivatives which are useful intermediates in the synthesis of taxol from baccatin III, said process comprises reacting an acyloxyacetyl halide with an imine derived from L-threonine; and to compounds of formula (III) which are produced in said process: ##STR1## wherein Ar is phenyl; R 1 is hydrogen, an acyl radical of a carboxylic acid, or a carbonic acid ester radical; R 2 is hydrogen or a carboxy protecting group; and R 3 is hydrogen or a hydroxy protecting group.
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.
专利号:WO-2018108954-A1 优先权日:2016-12-12 标题 :Process for the preparation of 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol 发明人:GOSSELIN FRANCIS; LINGHU XIN 权利人:HOFFMANN LA ROCHE; GENENTECH INC 摘要:Methods of making 2-(3-(fluoromethyl)azetidin-1-yl)ethan-1-ol 9, an intermediate useful for the synthesis of estrogen receptor modulating compounds are described.
专利号:US-5292891-A 优先权日:1991-02-21 标 题 :Optically active 2,2-dimethyl-1,3-dioxin-4-ones and method for preparing same and method for preparing optically active compound for synthesis of physiologically active substance and optically active intermediate compound 发明人:KANEKO CHIKARA; SATO MASAYUKI 权利人:CHISSO CORP 摘要:There are provided novel and optically active 2,2-dimethyl-1,3-dioxin-4-ones which are useful as starting materials for physiologically active compounds, functional materials or the like. Provided are optically active 5,6-epoxyhexanoic acid esters and novel optically active 6-substituted tetrahydropyran-2-one derivatives. That is, optically active 6-chloromethyltetrahydropyran-2-one can be synthesized by lactonizing optically active 2,2-dimethyl-6-(3-chloro-2-hydroxypropyl)-1,3-dioxin-4-one to form optically active 6-chloromethyltetrahydropyran-2,4-dione; reacting the thus formed compound with hydrogen in the presence of a catalyst to obtain optically active 6-chloromethyl-4-hydroxytetrahydropyran-2-one; subjecting this compound to a dehydration reaction, thereby obtaining optically active 6-chloromethyldihydropyran-2-one; reacting this compound with hydrogen in the presence of a catalyst to form optically active 6-chloromethyltetrahydropyran-2-one; and then treating this compound under basic conditions to prepare an optically active 5,6-epoxyhexanoic acid ester represented by the formula (6) ##STR1## (wherein the symbol * represents an asymmetric carbon atom, and R is a methyl group or an ethyl group).
专利号:US-6407255-B2 优先权日:1998-06-16 标题:Chemical synthesis of 1,2,4-triazolinone derivative 发明人:COTTRELL IAN FRANK; DOLLING ULF H; HANDS DAVID; WILSON ROBERT DARRIN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to a process for the preparation of morpholine derivatives of formula (I) which are useful as a therapeutic agents.
[参考文献]: Willem Van Brabandt, Et Al. Asymmetric Synthesis Of 1-(2- And 3-Haloalkyl)Azetidin-2-Ones As Precursors For Novel Piperazine, Morpholine, And 1,4-Diazepane Annulated Beta-Lactams. J Org Chem. 2006 Sep 1;71(18):7083-6.
合成参考文献
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