专利号:US-11485721-B2 优先权日:2017-11-21 标 题:Method for the metal-free preparation of a biaryl by a photosplicing reaction and their uses 发明人:KLOSS FLORIAN; NEUWIRTH TONI; HAENSCH VEIT; HERTWECK CHRISTIAN 权利人:LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST HKI; LEIBNIZ INST FUER NATURSTOFF FORSCHUNG UND INFEKTIONSBIOLOGIE E V HANS KNOELL INST 摘要:The present invention relates to a method for the metal-free preparation of a biaryl compound by a photosplicing reaction and its use in the preparation of chemical compounds, preferably of active ingredients e.g. in the fields of pharmaceuticals and agrochemicals. In particular, it refers to a method for the regiocontrolled preparation of a biaryl compound of formula (I): Ar—Ar′ by photochemically reacting a precursor compound of formula (II): Ar—L—Ar′ to form a biaryl compound of general formula: Ar—L—Ar′(II)→Ar—Ar′ (I) wherein Ar and Ar′, independently of each other, represent an unsubstituted or substituted C6-C20 aryl group or a heteroaryl group with 5-20 ring atoms selected from carbon, nitrogen, oxygen and sulfur, and L represents a group —X—Y—Z— as defined herein. The biaryl compounds are generally suitable as intermediates or key building blocks in a very broad spectrum of organic chemical syntheses and their respective utilities. Their use within the field of synthesis of active ingredients is an aspect of the invention, and their use in the preparation of pharmaceutically active ingredients is particularly preferred.
专利号:US-6326498-B1 优先权日:2001-03-13 标 题 :Process for the synthesis of 5-(2-flurophenyl)-1H-tetrazole 发明人:MALLADI PARDHASARADHI; KANTEVARI SRINIVAS; NAIR CHEMBUMKULAM KAMALAKSHYAM 权利人:COUNCIL SCIENT IND RES 摘要:The present invention discloses a process of the preparation of 5-(2-flurophenyl)-1H-tetrazole of the formula 2 by reacting 2-fluoro benzonitrile of the formula 1 n with an inorganic azide and an amine salt in an aromatic solvent, precipitating the product with hydrochloric acid and separating the precipitated product.
专利号:WO-2008012852-A1 优先权日:2006-07-27 标 题:Intermediate compounds for the preparation of angiotensin ii antagonists 发明人:GUANDALINI LUCA; MARTINI ELISABETTA; ROMANELLI MARIA NOVELLA; DALLATOMASINA FRANCO 权利人:S I M S S R L SOC IT MEDICINAL; GUANDALINI LUCA; MARTINI ELISABETTA; ROMANELLI MARIA NOVELLA; DALLATOMASINA FRANCO 摘要:The present invention relates to novel substituted biphenyltetrazole compounds useful as intermediates in the preparation of angiotensin II antagonists, to a process for the synthesis of them and to a process for the conversion thereof to said molecules.
专利号:WO-9637481-A1 优先权日:1995-05-26 标题:Novel reagent for tetrazole synthesis and process for producing tetrazoles therewith 发明人:TOKUHARA GINRO; YAMAGUCHI TADASHI; IWASAKI TETSUYA 权利人:CHUGOKU KAYAKU; WAKUNAGA SEIYAKU KK; TOKUHARA GINRO; YAMAGUCHI TADASHI; IWASAKI TETSUYA 摘要:A process for producing 1H-tetrazoles represented by general formula (II) (wherein R represents an arbitrary substituent) from carbonitriles represented by the general formula (I): R-CN (wherein R is as defined above) with the use of a tetrazolating agent comprising an alkali metal azide and zinc chloride. The agent can be used in a variety of solvents and can fundamentally be applied to any carbonitriles. As zinc chloride is inexpensive, it contributes to cost reduction.
专利号:US-6417400-B1 优先权日:1998-03-24 标题:Methyl-phenyl derivatives, preparation method and use 发明人:DORMOY JEAN-ROBERT; GOUBET DOMINIQUE; MOREAU PATRICE 权利人:SANOFI SYNTHELABO 摘要:The present invention relates to:a) methylbiphenyl derivatives of general formula:in which R1 represents OH, C3-C7 alkyl or C3-C7 cycloalkyl, these compounds being in the form of individual isomers or mixtures thereof,b) their preparation by reaction:either of a hydroxylamine salt with an N-substituted o-(p-tolyl)benzaldimine, to give o-(p-tolyl)benzaldoximeor of an N-substituted 2-halobenzaldimine with a p-tolylmagnesium halide in the presence of an inorganic manganese derivative, to give the compounds of formula I in which R1 represents C3-C7 alkyl or C3-C7 cycloalkylc) their use for the preparation of o-(p-tolyl)-benzonitrile, which is an intermediate in the synthesis of medicinal products.
专利号:US-7968727-B2 优先权日:2005-04-01 标 题 :Synthesis of 4-bromomethyl-2′-formylbiphenyl and 4-bromomethyl-2′-hydroxymethylbiphenyl and its use in preparation of angiotensin II antagonists 发明人:COPAR ANTON; ANTONCIC LJUBOMIR; ANTONCIC MATEJ 权利人:LEK PHARMACEUTICALS 摘要:4-bromomethyl-2′-formylbiphenyl and 4-bromomethyl-2′-hydroxymethylbiphenyl are useful starting material for the preparation various angiotenzin II antagonists, which are prepared from 4-bromomethyl-2′-cyanobiphenyl or 4′-bromomethylbiphenylcarboxyilic derivatives using selected hydride reagent.
参考标题:Synthesis Of Biaryls And Aryl KetonesViaMicrowave-Assisted Decarboxylative Cross-Couplings 作者:Lukas J. Gooßen,Bettina Zimmermann,Christophe Linder,Nuria Rodríguez,Paul P. Lange,Jens Hartung |发布日期:2009.11 摘要:A Protocol For The Microwave-Assisted Decarboxylative Cross-Couplings Of Carboxylic Acid Salts With Aryl Halides Has Been Developed That Allows The Synthesis Of Various Biaryls And Aryl Ketones In High Yields. After Careful Adaptation Of The Bimetallic Catalyst System And Reaction Conditions, These Mechanistically Complex Transformations Can Now Be Performed Within Only Five Minutes In Concentrated
合成参考文献
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