2',4'-二羟基-2-苯基苯乙酮置于吗啉,Potassium Carbonate体系中,用 N,N-二甲基甲酰胺,异丙醇 作为反应溶剂,化学反应 11.0H,反应生成 依普黄酮 参考文献:Synthesis Of Daidzin Analogues As Potential Agents For Alcohol Abuse 标题:Synthesis Of Daidzin Analogues As Potential Agents For Alcohol Abuse 摘要:Daidzin,The Active Principle Of An Herbal Remedy For 'Alcohol Addiction',Has Been Shown To Reduce Alcohol Consumption In All Laboratory Animals Tested To Date. Correlation Studies Using Structural Analogues Of Daidzin Suggests That It Acts By Raising The Monoamine Oxidase (Mao)/mitochondrial Aldehyde Dehydrogenase (Aldh-2) Activity Ratio (J. Med. Chem. 2000,43,4169). Structure-Activity Relationship (Sar) Studies On The 7-O-Substituted Analogues Of Daidzin Have Revealed Structural Features Important For Aldh-2 And Mao Inhibition (J. Med. Chem. 2001,44,3320). We Here Evaluated Effects Of Substitutions At 2,5,6,8,3' And 4' Positions Of Daidzin On Its Potencies For Aldh-2 And Mao Inhibition. Results Show That Analogues With 4'-Substituents That Are Small,Polar And With Hydrogen Bonding Capacities Are Most Potent Aldh-2 Inhibitors,Whereas Those That Are Non-Polar And With Electron Withdrawing Capacities Are Potent Mao Inhibitors. Analogues With A 5-Oh Group Are Less Potent Aldh-2 Inhibitors But Are More Potent Mao Inhibitors. All The 2-,6-,8-And 3'-Substituted Analogues Tested So Far Do Not Inhibit Aldh-2 And/or Have Decreased Potencies For Mao Inhibition. This,Together With The Results Obtained From Previous Studies,Suggests That A Potent Antidipsotropic Analogue Would Be A 4',7-Disubstituted Isoflavone. The 4'-Substituent Should Be Small,Polar,And With Hydrogen Bonding Capacities Such As,-Oh And-Nh2; Whereas The 7-Substituent Should Be A Straight-Chain Alkyl With A Terminal Polar Function Such As-(Ch2)(N)-Oh With 2 Less Than Or Equal To N Less Than Or Equal To 6,-(Ch2)(N)-Cooh With 5 Less Than Or Equal To N Less Than Or Equal To 10,Or-(Ch2)(N)-Nh2 With N Greater Than Or Equal To 4. (C) 2003 Elsevier Ltd. All Rights Reserved. DOI:10.1016/s0968-0896(03)00397-3
专利号:US-5286877-A 优先权日:1993-02-01 标 题:Synthesis of 1,4-dideoxy-1,4-imino-L-arabinitol 发明人:BEHLING JAMES R; MEDICH JOHN R; BABIAK KEVIN A; FLEET GEORGE W J 权利人:SEARLE & CO 摘要:1,4-Dideoxy-1,4-imino-L-arabinitol is chemically synthesized from D-lyxonolactone by formation of the pyrrolidine ring by joining the nitrogen between C-1 and C-4 and inversion of configuration at both C-2 and C-4, with the C-3 and C-5 hydroxyl groups being protected throughout the synthesis sequence by benzylidenation. The product is preferably isolated as the hydrochloride salt and is useful as an inhibitor of α-glucosidase and human immunodeficiency virus (HIV).
专利号:US-9169502-B2 优先权日:2010-06-15 标题 :Method of producing L-lysine using a Corynebacterium glutamicum microorganism 发明人:WITTMANN CHRISTOPH; BECKER JUDITH 权利人:WITTMANN CHRISTOPH; BECKER JUDITH; PAIK KWANG IND CO LTD 摘要:The present invention is directed to a method utilizing a recombinant microorganism for the production of aspartate derived amino acids and precursors thereof, in particular for the production of L-lysine. Furthermore, the present invention relates to a recombinant microorganism having improved aspartate-derived amino acid synthesis activity in comparison to the initial microorganism and the use of such microorganisms in producing said amino acids and precursors and derivatives, in particular in the synthesis of L-lysine.
专利号:US-2003157592-A1 优先权日:1999-12-16 标题:Moss genes from physcomitrella patens encoding proteins involved in the synthesis of tocopherols and carotenoids 发明人:LERCHL JENS; RENZ ANDREAS; EHRHARDT THOMAS; REINDL ANDREAS; CIRPUS PETRA; BISCHOFF FRIEDRICH; FRANK MARKUS; FREUND ANNETTE; DUWENIG ELKE; SCHMIDT RALF-MICHAEL; RESKI RALF; BADUR RALF 摘要:Isolated nucleic acid molecules, designated TCMRP nucleic acid molecules, which encode novel TCMRPs from e.g. Phycomitrella patens are described. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing TCMRP nucleic acid molecules, and host cells into which the expression vectors have been introduced. The invention still further provides isolated TCMRPs, mutated TCMRPs, fusion proteins, antigenic peptides and methods for the improvement of production of a desired compound from transformed cells, organisms or plants based on genetic engineering of TCMRP genes in these organisms.
专利号:US-7192749-B2 优先权日:2002-05-16 标题 :Use of the repressor glxR for the synthesis of lysine in Corynebacterium glutamicum 发明人:KLOPPROGGE CORINNA; ZELDER OSKAR; KROEGER BURKHARD; SCHROEDER HARTWIG; HAEFNER STEFAN; LEE HEUNG-SHICK 权利人:BASF AG 摘要:Isolated polypeptide sequence having the sequence of SEQ ID NO:1 or muteins thereof having the ability to bind cAMP and repress the expression of the aceB gene of C. glutamicum and which can be obtained from SEQ ID NO:1 by inserting, deleting or substituting up to 20% of the amino acids.
专利号:EP-1282713-A2 优先权日:1999-11-25 标 题 :Moss genes from physcomitrella patens encoding proteins involved in the synthesis of polyunsaturated fatty acids and lipids 发明人:LERCHL JENS; RENZ ANDREAS; EHRHARDT THOMAS; REINDL ANDREAS; CIRPUS PETRA; BISCHOFF FRIEDRICH; FRANK MARKUS; FREUND ANNETTE; DUWENIG ELKE; SCHMIDT RALF-MICHAEL; RESKI RALF 权利人:BASF PLANT SCIENCE GMBH 摘要:Isolated nucleic acid molecules, designated LMRP nucleic acid molecules, which encode novel LMRPs from e.g. Physcomitrella patens are described. The invention also provides antisense nucleic acid molecules, recombinant expression vectors containing LMRP nucleic acid molecules, and host cells into which the expression vectors have been introduced. The invention still further provides isolated LMRPs, mutated LMRPs, fusion proteins, antigenic peptides and methods for the improvement of production of a desired compound from transformed cells, organisms or plants based on genetic engineering of LMRP genes in these organisms.
专利号:US-5013842-A 优先权日:1990-01-22 标题:Synthesis of chiral pyrrolidine and piperidine glycosidase inhibitors 发明人:FLEET GEORGE W J; WITTY DAVID R 权利人:MONSANTO CO 摘要:There is disclosed a novel method for the syntheses of chiral pyrrolidines and piperidines by the intramolecular ring closure of anomeric mixtures of 4-amino- and 5-amino-2-trifluoromethanesulfonates of methyl furanosides. The novel method preferably provides for the efficient syntheses from diacetone glucose of 1,4-dideoxy-1,4-imino-D-arabinitol--known as DAB1, (2S,3R,4R)-3,4-dihydroxyproline, fagomine [1,5-imino-1,2,5-trideoxy-D-arabino-hexitol], and (2S,3R,4R)-3,4-dihydroxypipecolic acid by intramolecular nucleophilic displacement by an amino function of 2-O-trifluoromethanesulphonates of anomeric mixtures of methyl furanosides.