专利号:US-10011580-B2 优先权日:2016-04-21 标题:Diastereoselective synthesis of (±)-epianastrephin, (±)-anastrephin and analogs thereof 发明人:WALSE SPENCER S; KUZMICH DANIEL 权利人:US AGRICULTURE 摘要:A process for the synthesis of trans-fused γ-lactones having Formula (IV) from substituted cyclic ketones having Formula (I). A diastereoselective synthesis of (±)-epianastrephin (1) (wherein: R 1 is ethenyl, R 2 and R 3 is methyl, and n is 1), (±)-anastrephin (2) (wherein: R 2 is ethenyl, R 1 and R 3 is methyl and n is 1), and analogs thereof (wherein: R 1 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 2 is H, C 1-5 alkyl, C 2-6 alkenyl or C 2-6 alkynyl, R 1 and R 2 together with the carbon atom they are attached form a C 3-6 cycloalkyl ring, R 3 is C 1-5 alkyl and n is 0-2):
专利号:WO-9419366-A1 优先权日:1993-02-26 标题 :Chemical synthesis of squalamine 发明人:MORIARTY ROBERT M; GUO LIANG; TULADHAR SUDERSAN M 权利人:MAGAININ PHARMA 摘要:Methods for the chemical preparation or synthesis of the sterol antibiotic squalamine. Preferably, the preparation is by modifying the 3-position of a 3-oxo-7α-hydroxy-24z-ether protected alcohol group-5α-cholestane with a spermidino moiety to form a 3β-spermidino-7α-hydroxy-24z-ether protected group -5α-cholestane; deprotecting the 24-position of the 3β-spermidino-7α-hydroxy-24z-ether protected group-5α-cholestane to the free hydroxyl; and sulfating the 24-position of the 3β-spermidino-7α, 24-dihydroxy-5α-cholestane.
专利号:US-2010137659-A1 优先权日:2006-09-26 标题 :Process for the synthesis of 2,2',6-tribromobiphenyl 发明人:LEROUX FREDERIC; BONNAFOUX LAURENCE; COLOBERT FRANCOISE 权利人:LEROUX FREDERIC; BONNAFOUX LAURENCE; COLOBERT FRANCOISE 摘要:A process for the synthesis of 2,2′,6-tribromobiphenyl.
专利号:US-6814895-B2 优先权日:2000-12-20 标 题:Process for the synthesis of 1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-one 发明人:CVETOVICH RAYMOND; ASAI TOMOYUKI; YODOGAWA YOSHIKO 权利人:MERCK & CO INC 摘要:The present invention is concerned with a novel process for the preparation of 1-(3,5-bis(trifluoromethyl)phenyl)ethan-1-one (CAS 30071-93-3). This compound is useful as an intermediate in the synthesis of therapeutic agents.
专利号:US-10626102-B2 优先权日:2015-12-30 标题 :Process for the synthesis of efinaconazol 发明人:VERONESE MARTINO; BETTONI PIERGIORGIO; ROLETTO JACOPO; PAISSONI PAOLO 权利人:PROCOS SPA 摘要:Disclosed is a process for the synthesis of efinaconazole (I), starting from 1-[[(2R,3S)-2-(2,4-difluorophenyl)-3-methyloxiranyl]methyl]-1H-1,2,4-triazole and 4-methylenepiperidine, as free base or hydrochloride, in an organic solvent, under anhydrous conditions and in the presence of neutralising agents and reaction-promoting metal species. (1) The process is particularly advantageous because it gives rise to efinaconazole in high yields and purity, and uses little more than the stoichiometric amount of 4-methylenepiperidine, a rather expensive commercially available reagent.
专利号:US-4518813-A 优先权日:1981-10-02 标 题:Optically active units for the synthesis of the side chain of (R,R,R)-α-tocopherol and their preparation 发明人:ERNST HANSGEORG; VOGEL FRIEDRICH; PAUST JOACHIM 权利人:BASF AG 摘要:(2R,6R)-1-Chloro-2,6,10-trimethyl-undecane I, (R)-(+)-β-chloro-isobutyric acid II, (S)-(+)-1-bromo-3-chloro-2-methylpropane IV and (2R)-(+)-1-chloro-2,6-dimethyl-heptane V are novel optically active units for the synthesis of the side chain of (R,R,R)-α-tocopherol. In the process according to the invention, the optically active C 14 -chloride I is obtained in 6 simple reaction steps starting from II, via the novel intermediates IV and V, in accordance with the following equation: ##STR1##
参考标题:Organocerium Additions To Proline-Derived Hydrazones: Synthesis Of Enantiomerically Enriched Amines 作者:Scott E. Denmark,James P. Edwards,Theodor Weber,David W. Piotrowski |发布日期:2010.5 摘要:The Addition Of Organocerium Reagents (From Both Organolithium And Organomagnesium Precursors) To Chiral Aldehyde Hydrazones Prepared From 1-Aminoproline Derivatives Has Been Studied. The Additions Proceed In Good Yield And High Diastereoselectivity And With Good Nucleophile (Me, N-Bu, I-Pr, T-Bu, Ph, Etc.) And Substrate Scope (Alkyl, Alkenyl And Aryl). The Resulting Hydrazines Can Be Converted To
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