(3S,4S)-(-)-1-苄基-3,4-二羟基吡咯烷-2,5-二酮置于硼烷四氢呋喃络合物体系中,用 四氢呋喃 作为反应溶剂,化学反应 3.0H,以86.59%的收率获得产物(3S,4S)-1-苄基吡咯烷-3,4-二醇 参考文献:Synthesis And α-Glucosidase Inhibition Activity Of Dihydroxy Pyrrolidines 标题:Synthesis And α-Glucosidase Inhibition Activity Of Dihydroxy Pyrrolidines 摘要:A New Series Of Deacetylsarmentamide A And B Derivatives,Amides And Sulfonamides Of 3,4-Dihydroxypyrrolidines As Alpha-Glucosidase Inhibitors Were Designed And Synthesized. The Biological Screening Test Against Alpha-Glucosidase Showed That Some Of These Compounds Have The Positive Inhibitory Activity Against Alpha-Glucosidase. Saturated Aliphatic Amides Were More Potent Than The Olefinic Amides. Among All The Compounds,5O/6O Having Polar-Nh2 Group,10F/11F Having Polar-Oh Group On Phenyl Ring Displayed 3-4-Fold More Potent Than The Standard Drugs. Acarbose,Voglibose And Miglitol Were Used As Standard References. The Promising Compounds 6I,5O,6O,10A,11A,10F And 11F Have Been Identified. Molecular Docking Simulations Were Done For Compounds To Identify Important Binding Modes Responsible For Inhibition Activity Of Alpha-Glucosidase. (C) 2017 Elsevier Ltd. All Rights Reserved. DOI:10.1016/j.Bmcl.2017.04.078
专利号:US-2012289733-A1 优先权日:2011-05-11 标 题 :Novel borate derivatives and their applications 发明人:HEISE GLENN L; MYSLINSKA MALGORZATA 权利人:HEISE GLENN L; MYSLINSKA MALGORZATA; ANDERSON DEV CO 摘要:Borates, compositions comprising chiral (cyclic and acyclic) and achiral (cyclic and acyclic) borates; chiral (cyclic and acyclic) and achiral (cyclic and acyclic) biborates; and methods for their synthesis. Additionally, a significantly improved synthetic protocol for the synthesis of wide range of boronates starting from borates or biborates and Grignard or organolithium reagents that can be used for kilo lab and commercial scale production.
专利号:US-2010022549-A1 优先权日:2008-07-23 标题 :Alpha-helix mimetic with functionalized pyridazine 发明人:REBEK JR JULIUS; MOISAN LIONEL; CARELLA ALEXANDRE; MANN ENRIQUE 权利人:SCRIPPS RESEARCH INST 摘要:The synthesis of new α-helix scaffolds mimicking i, i+3 or i+4, i+7 residues, was accomplished. The common pyridazine heterocycle originates from the easily available dimethyl pyridazine-3,6-dicarboxylate building block. These scaffolds may be thought of as synthetic counterparts of amphiphilic α-helices having a hydrophilic face along one side and a hydrophobic face along the other side of the helix.
专利号:US-6090950-A 优先权日:1996-08-23 标 题 :Chiral hydride complexes 发明人:HEISE GLENN L 权利人:ZEELAND CHEMICALS INC 摘要:Novel chiral boron and aluminum hydride complexes, compositions comprising the chiral hydride complexes, and methods for their synthesis and use are described. The novel chiral hydride complexes are of the formulas: MBH4-n-a(R*)n(R')a; MBH2-b(R**) (R')b; MBH(R***); MBH(R*) (R''); MAlH4-n-a(R*)n(R')a; MAlH2-b(R**)(R')b; MAlH(R***); and MAlH(R*) (R''), wherein M is Na+, Li+ or K+; each R* is independently a monodentate chiral ligand; R** is a bidentate chiral ligand; R*** is a tridentate chiral ligand; R' is a monodentate achiral ligand; R'' is a bidentate achiral ligand; n is 1-3; a is 0-2; and b is 0-1, with the proviso that n+a=3, and with the further proviso that when R** is S-BINOL, M is not Li+.
参考文献:10.1055/s-2007-965914 摘要:Brandi A, Revuelta J, Cicchi S, Goti A. Enantiopure Cyclic Nitrones: A Useful Class of Building Blocks for Asymmetric Syntheses. Synthesis. 2007 Jan 29;2007(04):485–504. doi: 10.1055/s-2007-965914. 参考文献:10.1055/s-0036-1588569 摘要:Shaw A, Ajay S. Studies Towards the Synthesis of (+)- and (–)-Anisomycin and Their Analogues. Synthesis. 2017 Oct 04;50(01):17–34. doi: 10.1055/s-0036-1588569. 参考文献:10.1055/s-0028-1087950 摘要:Cardona F, Bonanni M, Soldaini G, Faggi C, Goti A. Novel l-Tartaric Acid Derived Pyrrolidinium Cations for the Synthesis of Chiral Ionic Liquids. Synlett. 2009 Feb 24;2009(05):747–50. doi: 10.1055/s-0028-1087950. 参考文献:10.1055/s-0029-1218622 摘要:Wünsch B, Fricke Y, Kopp N. Synthesis of Iminodiacetaldehyde Derivatives as Building Blocks for Pharmacologically Active Agents. Synthesis. 2010 Jan 08;2010(05):791–6. doi: 10.1055/s-0029-1218622.