[EN] CLASS OF HETEROAROMATIC COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF [FR] CLASSE D'UN COMPOSÉ HÉTÉROAROMATIQUE, SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION [ZH] 一类芳杂环类化合物及其制备方法和用途
We report the synthesis of 2-(anthracen-9-yl)-1H-inden-3-yl dicyclohexylphosphine and its use in palladium-catalyzed borylation/Suzuki-Miyauracross-coupling reaction to prepare a variety of symmetrical and unsymmetrical biaryl compounds in excellent yield.
Scope of the Two-Step, One-Pot Palladium-Catalyzed Borylation/Suzuki Cross-Coupling Reaction Utilizing Bis-Boronic Acid
作者:Gary A. Molander、Sarah L. J. Trice、Steven M. Kennedy
DOI:10.1021/jo301642v
日期:2012.10.5
synthesis of boronic acids has greatly facilitated the two-step, one-potborylation/Suzukicross-couplingreaction between aryl and heteroaryl halides. With use of Buchwald’s second-generation XPhos preformed catalyst, high yields of cross-coupled products were obtained for most substrates. The method also allows an efficient two-step, one-pot synthesis, providing access to three distinct cross-coupled
Decarbonylative Pd-Catalyzed Suzuki Cross-Coupling for the Synthesis of Structurally Diverse Heterobiaryls
作者:Alejandro Cervantes-Reyes、Aaron C. Smith、Gary M. Chinigo、David C. Blakemore、Michal Szostak
DOI:10.1021/acs.orglett.2c00267
日期:2022.3.4
Heteroaromatic biaryls are core scaffolds found in a plethora of pharmaceuticals; however, their direct synthesis by the Suzuki cross-coupling is limited to heteroaromatic halide starting materials. Here, we report a direct synthesis of diverse nitrogen-containing heteroaromatic biaryls by Pd-catalyzed decarbonylative Suzuki cross-coupling of widely available heterocyclic carboxylic acids with arylboronic
[EN] SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY<br/>[FR] DIHYDROPYRIMIDINONES BICYCLIQUES SUBSTITUÉES ET LEUR UTILISATION EN TANT QU'INHIBITEURS DE L'ACTIVITÉ DE L'ÉLASTASE NEUTROPHILE
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2016016364A1
公开(公告)日:2016-02-04
This invention relates to substituted bicyclic dihydropyrimidinones of formula 1 and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.
SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
申请人:Boehringer Ingelheim International GmbH
公开号:EP3604308A1
公开(公告)日:2020-02-05
This invention relates to substituted bicyclic dihydropyrimidinones of formula 1
and their use as inhibitors of neutrophil elastase activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of pulmonary, gastrointestinal and genitourinary diseases, inflammatory diseases of the skin and the eye and other autoimmune and allergic disorders, allograft rejection, and oncological diseases.