专利号:US-4336383-A 优先权日:1980-05-07 标题:1-1-Binaphthyl-4,4',5,5',8,8'-hexacarboxylic acid compounds, method of preparation and use thereof for the synthesis of asymmetric derivatives of 3,4,9,10-perylenetetracarboxylic acid, and for dyeing and printing of textile materials 发明人:VOROZHTSOV GEORGY N; MASANOVA NATALIA N; FELDBLJUM NIKOLAI B; ALEXEEV VASILY I; SHIGALEVSKY VADIM A; SOLOMATIN GEORGY G; SHULEPOVA OLGA I; KHAITUN GALINA G; GORDEEVA NADEZHDA V 权利人:VOROZHTSOV GEORGY N; MASANOVA NATALIA N; FELDBLJUM NIKOLAI B; ALEXEEV VASILY I; SHIGALEVSKY VADIM A; SOLOMATIN GEORGY G; SHULEPOVA OLGA I; KHAITUN GALINA G; GORDEEVA NADEZHDA V 摘要:1,1'-Binaphthyl-4,4',5,5',8,8'-hexacarboxylic acid compounds having the following formula: ##STR1## wherein R 1 is hydrogen, halogen, or alkyl; when X is oxygen, Y is hydrogen, alkyl, a cycloalkyl, or an aryl containing at least one substituent from the group including: halogen, alkyl, or alkoxy, when X is nitrogen, Y is ##STR2## wherein R 2 is hydrogen, halogen, or alkyl; Y being linked to X with the formation of a benzimidazole cycle. n The method for preparing the compounds according to the present invention resides in the treatment of that 1,1'-binaphthyl-4,4',5,5',8,8'-hexacarboxylic acid anhydride with an alkali to give a corresponding salt which is condensed with orthophenylenediamines upon heating at reflux at a pH of from 6.3 to 6.8. The resulting benzimidazole-1,1'-binaphthyl-4,4',5,5',8,8'-hexacarboxylic acid anhydride having the formula: ##STR3## wherein R 1 is hydrogen, halogen, or alkyl, is isolated and condensed with an amine or ortho-phenylenediamines in an excess of the amine, in water or an organic solvent, followed by isolation of the desired product. n The compounds according to the present invention are employed for the synthesis of asymmetric compounds of 3,4,9,10-perylenetetracarboxylic acid, as well as for dyeing and printing of textile materials with the formation, on the material, of asymmetric compounds of 3,4,9,10-perylenetetracarboxylic acid having the following formula: ##STR4## wherein R 1 is hydrogen, halogen, or alkyl; when X is oxygen, Y is hydrogen, alkyl, cycloalkyl, or aryl containing at least one substituent from the group including; halogen, alkyl, or alkoxy, when X is nitrogen, Y is ##STR5## where R 2 is hydrogen, halogen, or alkyl; Y being linked with X to form a benzimidazole cycle. n The compounds according to the present invention dye textile materials to various shades of violet color.
专利号:US-8895741-B2 优先权日:2003-06-03 标 题:Process for the synthesis of biaryl oxazolidinones 发明人:WU YUSHENG; CHEN SHILI; CHEN YI; HANSELMANN ROGER; LOU RONGLIANG; ZHOU JIACHENG 权利人:WU YUSHENG; CHEN SHILI; CHEN YI; HANSELMANN ROGER; LOU RONGLIANG; ZHOU JIACHENG; MELINTA THERAPEUTICS INC 摘要:The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
专利号:US-5693792-A 优先权日:1992-02-18 标 题 :β-lactam and cephem compounds and processes for their production 发明人:TORII SHIGERU; TANAKA HIDEO; SASAOKA MITIO; SHIROI TAKASHI; KAMEYAMA YUTAKA 权利人:OTSUKA KAGAKU KK 摘要:The object of the invention is to provide a β-lactam compound and a 2-substituted methyl-3-cephem compound, both of which are of value as intermediates for the synthesis of cephem antibiotics. n The β-lactam compound of the invention may be represented by the general formula ##STR1## wherein R 1 represents a protected amino group, for instance; R 2 represents hydrogen, for instance; R 3 represents hydrogen or a carboxy-protecting group; R 4 represents an aryl group which may be substituted; R 5 represents an alkenyl group which may be substituted, for instance. The 2-substituted methyl-3-cephem compound of the invention may be represented by the general formula ##STR2## wherein R 1 , R 2 and R 3 are as defined above; R 6 represents an aryl group which may be substituted.
专利号:US-7517895-B2 优先权日:2001-08-24 标题 :Synthetic diazonamides 发明人:HARRAN PATRICK G; LI JING; JEONG SUSAN 权利人:UNIV TEXAS 摘要:The application discloses novel synthetic compounds, modeled after unique toxins extracted from the marine invertebrate Diazona angulata useful in the treatment abnormal cell mitosis. The application also discloses novel methods for synthesis of these compounds and methods of using these compounds.
专利号:US-12180188-B2 优先权日:2020-05-19 标题:Antifibrotic compounds and related methods 发明人:STEFANOVIC BRANKO; NEFZI ADEL 权利人:UNIV FLORIDA STATE RES FOUND; THE FLORIDA INTERNATIONAL UNIV BOARD OF TRUSTEES 摘要:This discloses that compounds of Formula 1 have antifibrotic properties. In particular, this discloses a pharmaceutical composition including one or more compounds of Formula 1 and methods of using compounds of Formula 1 in fibrosis treatment and inhibiting type 1 collagen synthesis.
专利号:US-7612064-B2 优先权日:2003-05-26 标题:Sulfopyrroles 发明人:EBERLE MARTIN; ERMERT PHILIPP; OBRECHT DANIEL; LACH FRANK; LUTHER ANATOL; BACHMANN FELIX; STREBEL ALLESSANDRO 权利人:TAKEDA PHARMACEUTICAL 摘要:The invention relates to compounds of formula (I) wherein R 1 represents aryl, aralkyl or heteroaryl, R 2 is aryl or heteroaryl and R 3 is aryl, heteroaryl or optionally substituted aminomethyl, to methods of synthesis of such compounds, to pharmaceutical compositions containing compounds of formula (I), to the use of a compounds of formula (I) for the preparation of a pharmaceutical composition for the treatment of neoplastic and autoimmune diseases, and to methods of treatment of neoplastic and autoimmune diseases using compounds of formula (I) or of pharmaceutical compositions containing same.
参考标题:A Novel Oxidative Procedure For The Synthesis Of Benzamides From Styrenes And Amines Under Metal-Free Conditions 作者:Muhammad Sharif,Jin-Long Gong,Peter Langer,Matthias Beller,Xiao-Feng Wu 摘要:An Interesting Procedure For The Oxidative Synthesis Of Amides From Styrenes And Amines Has Been Developed. Various Primary Amides Were Formed In Moderate Yields (25-81%). Secondary Amides Can Be Produced In Moderate Yields As Well (41-68%). Notably, No Transition Metal Catalyst Was Needed For This Transformation. This Is The First Example Of Oxidative Transformation Of Styrenes To Benzamides.
合成参考文献
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