📜1-碘-3,4-亚甲基二氧基苯,(R)-6-((E)-2-(Tributylstannyl)Vinyl)-5,6-Dihydro-4-Methoxypyran-2-One置于tris(Dibenzylideneacetone)Dipalladium (0) 三(2-呋喃基)膦体系中,用 甲苯 作为反应溶剂,以44%的收率获得产物麻醉椒苦素 参考文献:Versatile Asymmetric Synthesis Of The Kavalactones: First Synthesis Of (+)-Kavain 标题:Versatile Asymmetric Synthesis Of The Kavalactones: First Synthesis Of (+)-Kavain 摘要:Three Asymmetric Pathways To The Kavalactones Have Been Developed. The First Method Is Chiral Auxiliary-Based And Utilizes Aldol Reactions Of N-Acetyl Thiazolidinethiones Followed By A Malonate Displacement/decarboxylation Reaction. The Second Approach Uses The Asymmetric Catalytic Mukaiyama Additions Of Dienolate Nucleophile Equivalents Developed By Carreira And Sato. Finally,Tin-Substituted Intermediates,Prepared By Either Of These Routes,Can Serve As Advanced General Precursors Of Kavalactone Derivatives Via Pd(0)-Catalyzed Stille Couplings With Aryl Halides. DOI:10.1021/ol0493960
专利号:US-11746364-B2 优先权日:2018-01-17 标题 :Enzymatic synthesis of kavalactones and flavokavains 发明人:PLUSKAL TOMÃ?S; Weng jing-ke 权利人:WHITEHEAD INST BIOMEDICAL RES 摘要:Disclosed are methods, compositions, proteins, nucleic acids, cells, vectors, compounds, reagents, and systems for the preparation of kavalactones, flavokavains, and kavalactone and flavokavain biosynthetic intermediates using enzymes expressed in heterologous host cells, such as microorganisms or plants, or using in vitro enzymatic reactions. This invention also provides for the expression of the enzymes by recombinant cell lines and vectors. Furthermore, the enzymes can be components of constructs such as fusion proteins. The kavalactones produced can be utilized to treat anxiety disorder, insomnia, and other psychological and neurological disorders. The flavokavains produced can be utilized to treat various cancers including colon, bladder, and breast cancers.
专利号:US-6677462-B2 优先权日:2001-08-06 标题:Asymmetric synthesis of kavalactones 发明人:CHEN SHOUJUN; SUN LIJUN; MCCLEARY JOEL 权利人:KAVA PHARMACEUTICALS INC 摘要:This invention relates to preparation of enantio-enriched compounds, and more particularly to enantio-enriched kavalactone compounds and derivatives thereof. The methods provide compounds that are useful as reagents, or building blocks, in the construction of other enantio-enriched compounds.
专利号:US-2019271015-A1 优先权日:2018-01-17 标题 :Enzymatic synthesis of kavalactones and flavokavains
专利号:US-10941429-B2 优先权日:2018-01-17 标 题:Enzymatic synthesis of kavalactones and flavokavains
专利号:CA-2456720-A1 优先权日:2001-08-06 标题 :Asymmetric synthesis of kavalactones
专利号:EP-1414463-A4 优先权日:2001-08-06 标题 :ASYMMETRIC SYNTHESIS OF KAVALACTONES
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合成参考文献
参考文献:10.1248/bpb.29.834 摘要:Matsuda H, Hirata N, Kawaguchi Y, Naruto S, Takata T, Oyama M, Iinuma M, Kubo M. Melanogenesis Stimulation in Murine B16 Melanoma Cells by Kava (Piper methysticum) Rhizome Extract and Kavalactones. Biological & Pharmaceutical Bulletin. 2006;29(4):834–7. doi: 10.1248/bpb.29.834.