专利号:US-10308588-B2 优先权日:2014-12-15 标 题 :Synthesis of amides and amines from aldehydes or ketones by heterogeneous metal catalysis 发明人:CÓRDOVA ARMANDO; PALO-NIETO CARLOS; AFEWERKI SAMSON 权利人:ORGANOFUEL SWEDEN AB 摘要:A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.
专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:WO-2024153752-A1 优先权日:2023-01-20 标 题 :Stereoselective synthesis of intermediates and synthesis of quinagolids 发明人:RYBERG PER; PINESCHI MAURO; COMPARINI LUCREZIA 权利人:FERRING BV 摘要:Disclosed is a method for preparing compounds with improved stereoselectivities. The described compounds are useful intermediates and may find particular application in the synthesis of compounds containing an octahydrobenzoquinoline moiety (e.g. an octahydrobenzo[g]quinoline moiety), such as quinagolide and its derivatives. Also disclosed is a method for stereoselectively (e.g. enantioselectively) preparing an intermediate used in the existing manufacturing process for the synthesis of quinagolide this intermediate also finding utility in the synthesis of other compounds containing an octahydrobenzo[g]quinoline moiety, in particular those having a substituent at the 3- position on the octahydrobenzo[g]quinoline.
专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-12344881-B2 优先权日:2023-09-27 标题 :Genetic engineering bacterium for de novo synthesis of cis,cis-muconic acid by taking glucose as substrate and applications thereof 发明人:TAN TIANWEI; LI MENGLEI 权利人:UNIV BEIJING CHEM TECH 摘要:The present invention discloses a genetic engineering bacterium for de novo synthesis of cis,cis-muconic acid by taking glucose as a substrate and applications thereof, and belongs to the technical field of genetic recombination and metabolic engineering. The genetic engineering bacterium for de novo synthesis of cis,cis-muconic acid (MA) by taking glucose as the substrate disclosed in the present invention is modified with chassis microbes, and includes recombinant Corynebacterium glutamicum for a cis,cis-muconic acid pathway construction module and an intermediate high-yield module. Production capacity of strains is greatly improved; MA of 90.2 g/L is finally obtained in fermentation liquor; and possibilities are provided for green and low-cost production of numerous chemicals such as adipic acid and nylon-66.
专利号:US-11220513-B2 优先权日:2015-04-30 标题:Chromium-mediated coupling and application to the synthesis of halichondrins 发明人:KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO 权利人:HARVARD COLLEGE 摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
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合成参考文献
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