三异丙基甲硅烷基吡咯-2-羧酸酯置于四丁基氟化铵体系中,用86%的收率获得产物吡咯-2-羧酸 参考文献:N-(Triisopropylsilyl)Pyrrole. A Progenitor "Par Excellence" Of 3-Substituted Pyrroles 标题:N-(Triisopropylsilyl)Pyrrole. A Progenitor "Par Excellence" Of 3-Substituted Pyrroles 摘要:A Very Effective Strategy Has Been Devised For The Synthesis Of 3-Substituted Pyrroles Based On The Use Of The Triisopropylsilyl (Tips) Moiety As A Sterically Demanding Nitrogen Substituent To Obstruct The Attack Of Electrophilic Reagents At The Alpha-Positions. 1-(Triisopropylsilyl)Pyrrole (1) Undergoes Highly Preferential Kinetic Electrophilic Substitution At The Beta-Position With A Variety Of Electrophiles (Br+,I+,No2+,Rco+,Etc.) And Fluoride Ion Induced Desilylation Of The Products Provides The Corresponding 3-Substituted Pyrroles In Good Overall Yields. Competitive Trifluoroacetylation Experiments Demonstrate That Substitution Of Tips-Pyrrole At The Alpha-Positions Is Decelerated By A Factor Of > 10(4),Vs Pyrrole At The Same Sites,Without Affecting Reactivity At The Beta-Positions. 1-(Triisopropylsilyl)-3-Bromopyrrole (2) Is Readily Converted Into The 3-Lithio Compound 44 By Bromine-Lithium Interchange With Alkyllithium Reagents. This Previously Unavailable,Formal Equivalent Of 3-Lithiopyrrole Is Itself An Excellent Source Of A Wide Range Of Beta-Substituted Pyrroles,Many Of Which Would Not Be Directly Preparable From 1. Tips-Pyrrole Can Be 3,4-Dihalogenated And These Compounds Undergo Sequential Halogen-Metal Interchange Trapping Reactions. This Process Is Exemplified By An Efficient,Three-Step Synthesis Of The Antibiotic Verrucarin E (63) From The Dibromo Compound 5. DOI:10.1021/jo00313A019
专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-10919904-B2 优先权日:2016-08-17 标 题 :Northern-southern route to synthesis of bacteriochlorins 发明人:LIU YIZHOU; LINDSEY JONATHAN S; ALLU SRINIVASA RAO; FUJITA HIKARU 权利人:UNIV NORTH CAROLINA STATE 摘要:Described herein are chlorins, bacteriochlorins, methods and intermediates for the synthesis of bacteriochlorins, and methods of using such bacteriochlorins for, among other things, diagnostic and therapeutic purposes such as luminescent compounds in flow cytometry, and as active agents in photodynamic therapy (PDT).
专利号:WO-2017089470-A1 优先权日:2015-11-27 标 题:Process for the synthesis of aryldiazonium salts using nitrogen oxides in oxygen-containing gas streams, especially from industrial waste gases 发明人:HOFMANN DAGMAR; HOFMANN JOSEFA; HEINRICH MARKUS 权利人:Friedrich-Alexander-Universität Erlangen-Nürnberg 摘要:The present invention relates to a process for the synthesis of aryldiazonium salts using nitrogen oxides in oxygen-containing gas streams, especially from industrial waste gases.
专利号:US-2013338369-A1 优先权日:2011-03-07 标 题 :Process for the Synthesis of Aminobiphenylene 发明人:HEINRICH MARKUS; PRATSCH GERALD 权利人:HEINRICH MARKUS; PRATSCH GERALD; BASF SE 摘要:The present invention relates to a process for the synthesis of 2-aminobiphenylene and derivatives thereof by reacting a benzene diazonium salt with an aniline compound under basic reaction conditions.
专利号:US-10005720-B2 优先权日:2013-04-05 标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same 发明人:SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L 权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL 摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.
摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 119. 摘要:Hay, M. B.; Hicks, J. D., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 113. 摘要:C. M. McCay and C. L. A. Schmidt. J. Gen. Physiol. 9, 333 (1926). 摘要:M. Scrocco and R. Nicolaus, Atti accad. naz. Lincei, Rend. Classe sci. fis. mat. e nat. 22, 311 (1957); CA 52, 50i. 摘要:P. Lumme, Suom. Kemistil. B 33, 87 (1960).