专利号:WO-0208446-A9 优先权日:2000-07-13 标题 :Synthesis and antiviral evaluation of nucleic acid based (nab) libraries 发明人:IYER RADHAKRISHNAN P; ZHOU WENQIANG; JIN YI; ROLAND ARLENE; LYAKU JAPHET 权利人:ORIGENIX TECHNOLOGIES INC 摘要:The present invention provides for compositions and methods to generate a library of small molecules that mimic the repertoire of interactions that exist amongst nucleic acids, and proteins, as well as, that which exist between proteins and nucleic acids. The designed library of nucleoside analogs are for use as competitive and non-competitive viral replication inhibitors or serve as pro-drugs of inhibitors in anti-viral drug discovery. A facile parallel solution-phase chemistry has been developed to carry out the combinatorial synthesis of nucleoside analogs as a source of pharmacore-based chemical diversity.
专利号:EP-0067342-A1 优先权日:1981-06-04 标 题 :Process for the preparation of 2-chloro-1,3-dimethoxybenzene 发明人:SHUTSKE GREGORY MICHAEL; LEE THOMAS BING KIN DR; JOBIN GREGORY MICHAEL 权利人:HOECHST ROUSSEL PHARMA 摘要:An improved process for the preparation of 2-chloro-1,3-dimethoxybenzene involving the conversion of 1,3-dimethoxybenzene to [2,6-dimethoxyphenyl]-lithium and the reaction of this compound with a chlorinating agent is disclosed. 2-Chloro-1,3-dimethoxybenzene is useful as starting material for the synthesis of pharmacologically valuable 1,2-benzisoxazoloxy acetic acids.
专利号:US-4579981-A 优先权日:1981-06-04 标题:Process for the preparation of 2-chloro-1,3-dimethoxybenzene 发明人:SHUTSKE GREGORY M; LEE THOMAS B K; JOBIN GREGORY M 权利人:HOECHST ROUSSEL PHARMA 摘要:An improved process for the preparation of 2-chloro-1,3-dimethoxybenzene involving the reaction of [2,6-dimethoxyphenyl]lithium with chlorinating agents is disclosed. 2-Chloro-1,3-dimethoxybenzene is useful as a starting material for the synthesis of pharmacologically valuable 1,2-benzisoxazoloxyacetic acids.
专利号:US-9890125-B2 优先权日:2013-01-08 标 题:Syntheses of N-heterocyclic carbenes and intermediates therefor 发明人:NOLAN STEVEN P; MEIRIES SEBASTIEN 权利人:UNIV COURT UNIV ST ANDREWS 摘要:A method of preparing a 2,6 disubstituted anilines includes, reacting a 2-amino isophthalic acid diester with sufficient Grignard reagent R 2 CH 2 MgX to form the corresponding diol product, dehydrating the diol product to the corresponding dialkene; and hydrogenating the diol product to form the corresponding aniline. The 2,6 disubstituted anilines can be used to produce N-Heterocyclic Carbenes (NHCs). The NHCs can find application in various fields such as organic synthesis, catalysis and macromolecular chemistry. Palladium catalysts containing the NHCs are also described.
专利号:US-9006491-B2 优先权日:2009-10-22 标题 :Structure and method for synthesizing and using dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate 发明人:MA SHENGMING; LÜ BO; FU CHUNLING 权利人:MA SHENGMING; LÜ BO; FU CHUNLING; UNIV ZHEJIANG 摘要:The current invention relates to the structure, synthesis of dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate, as well as its applications in the palladium catalyzed carbon-chlorine bond activation for Suzuki coupling reactions and carbon-nitrogen bond formation reactions. The dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine or its tetrafluoroborate could coordinate with the palladium catalyst to activate the inert carbon-chlorine bond highly selectively and catalyze Suzuki coupling reaction with arylboronic acid or carbon-nitrogen bond formation reaction with organic amines. The current invention uses only one step to synthesize dialkyl(2,4,6- or 2,6-alkoxyphenyl)phosphine and its tetrafluoroborate is stable in the air. Compared with known synthetic routes of ligands used in activating carbon-chlorine bonds, the method of current invention is short, easy to operate. Moreover, with this type of ligands, the Suzuki coupling products of optically active chlorolactones and arylboronic acids would maintain their configuration and optical purity.
专利号:JP-7199401-B2 优先权日:2013-01-08 标题:Synthesis of N-heterocyclic carbenes and their intermediates
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