📜(E)-Pent-1-En-1-Yl-1,3,2-Benzodioxaborole置于水体系中,化学反应 1.0H,以87%的收率获得1-戊烯基硼酸 参考文献:2-Pyrones Possessing Antimicrobial And Cytotoxic Activities 标题:2-Pyrones Possessing Antimicrobial And Cytotoxic Activities 摘要:The 2-Pyrone Sub-Unit Is Found In A Number Of Natural Products Possessing Broad Spectrum Biological Activity. Such Compounds Are Validated As Being Capable Of Binding To Specific Protein Domains And Able To Exert A Remarkable Range Of Biological Effects. In An Effort To Identify Synthetic 2-Pyrones With Interesting Biological Effects,Herein We Report The Synthesis And Biological Evaluation Of 4-Substituted-6-Methyl-2-Pyrones. Synthetic Routes To 4-Alkyl/alkenyl/aryl/alkynyl-6-Methyl-2-Pyrones Have Been Developed Utilising Sonogashira,Suzuki And Negishi Cross-Coupling Starting From Readily Available 4-Bromo-6-Methyl-2-Pyrone. Specific Conditions For Each Organometallic Protocol Were Required For Successful Cross-Coupling. In Particular,A Triethylamine/acetonitrile-Base/solvent Mixture Was Crucial To Sonogashira Alkynylation Of 4-Bromo-6-Methyl-2-Pyrone,Whereas Thallium Carbonate Was A Mandatory Base For The Suzuki Cross-Coupling Of Trialkylboranes. The 2-Pyrones Demonstrate Potent Inhibitory Activity Against Bacillus Subtilis,Escherichia Coli,Staphylococcus Aureus,Schizosaccharomyces Pombe And Botrytis Cinerea. The Growth Inhibitory Activities Of Selected 2-Pyrones Were Determined In A2780 Human Ovarian Carcinoma And K562 Human Chronic Myelogenous Leukaemia Cell Lines Using An In Vitro Cell Culture System (Mtt Assay). These Studies Demonstrate That 4-Phenylethynyl-,4-Tetrahydropyranylpropargyl Ether-And 4-Ethynyl-6-Methyl-2-Pyrones Have Excellent Potential As A New Class Of Anticancer Agents. (C) 2004 Elsevier Ltd. All Rights Reserved. Doi:10.1016/j.Bmc.2004.01.051
专利信息
专利号:US-8207337-B2 优先权日:2007-01-29 标 题:Reagent for organic synthesis reaction containing organic triol borate salt 发明人:MIYAURA NORIO; YAMAMOTO YASUNORI 权利人:MIYAURA NORIO; YAMAMOTO YASUNORI; WAKO PURE CHEM IND LTD 摘要:[Problem] n To provide an organoboron compound-containing reagent for organic synthesis reactions which undergoes no trimerization with dehydration, does not necessitate activation with a base, and is stable and highly active. n [Means for Solving Problems] n The reagent for organic synthesis reactions contains an organic triol borate salt represented by any of the general formulae (I) to (III) and general formula (XVI): (wherein R 1 represents alkyl, alkenyl, etc.; R 2 represents optionally substituted alkyl, alkenyl, alkynyl, etc. or represents hydrogen; m + represents an alkaline metal ion, phosphonium ion, or given ammonium ion; M 2+ represents an alkaline earth metal; X represents halogen or alkoxide; Y represents an alkali metal ion, etc.; A represents optionally substituted methylene; and n represents an integer).
专利号:WO-2008022467-A1 优先权日:2006-08-25 标 题 :2-substituted azain doles and 2 substituted thienopyrroles, their precursors and novel processes for the preparation thereof 发明人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING 权利人:LAUTENS MARK; YUEN JOSEPHINE; FANG YUANQING 摘要:The present invention relates generally to processes for the chemical synthesis of azaindole and thienopyrrole compounds, in particular azaindole and thienopyrrole compounds that are substituted at the 2-position of the azaindole or thienopyrrole ring, and optionally at additional locations of the azaindole or thienopyrrole ring such as the 1- and/or 3-position, compounds prepared by such processes, and synthetic precursors of such processes. More particularly, the present invention relates to the preparation of 2- substituted azaindoles from an ortho-gem-dihalovinylaminopyridine or from an ortho- gem-dihalovinylaminopyridine N-oxide compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to the preparation of 2-substituted thienopyrroles from an ortho-gem-dihalovinylthiophene compound and an organoboron reagent using a palladium metal pre-catalyst, base and a ligand. The present invention also relates to processes for the production of ortho-gem- dihalovinylaminopyridines which are useful as starting materials in the production of 2- substituted azaindoles, and novel compounds prepared by the processes. The present invention also relates to processes for the production of ortho-gem-dihalovinylthiophenes which are useful as starting materials in the production of 2-substituted thienopyrroles, and novel compounds prepared by the processes. Formulae (V) and (VII).
专利号:CN-114634407-A 优先权日:2020-12-16 标题 :A kind of method for stereospecific synthesis of 2-alkenal, 2-enone compound and deuterated compound thereof
专利号:CN-114634407-B 优先权日:2020-12-16 标题:A method for stereospecific synthesis of 2-enal, 2-enone compounds and their deuterated compounds
专利号:WO-2022127712-A1 优先权日:2020-12-16 标题 :Method for stereospecific synthesis of 2-enal and 2-enone compounds, and deuterated compounds thereof