Synthesis of C1-Substituted Oxabenzonorbornadienes
摘要:
Oxabenzonorbornadienes are valuable synthetic intermediates because they can serve as a general template with which to create highly substituted ring systems. However, to date, only very few C1-substituted oxabenzonorbornadienes have been reported. In this study, the synthesis of some C1-substituted oxabenzonorbornadienes was achieved by the Diels-Alder reaction between 2-substituted furans and benzyne. Moderate to good yields (16-80%) of the Diels-Alder reactions were observed. These C1-substituted oxabenzonorbornadienes will find applications as valuable synthetic intermediates and should be useful in studies of transition-metal-catalyzed reactions.
SUBSTITUTED BICYCLIC DIHYDROPYRIMIDINONES AND THEIR USE AS INHIBITORS OF NEUTROPHIL ELASTASE ACTIVITY
申请人:Boehringer Ingelheim International GmbH
公开号:US20160031830A1
公开(公告)日:2016-02-04
Substituted dihydropyrimidinones of formula 1
which are neutrophil elastase inhibitors and useful as medicaments for the treatment of, inter alia, COPD. Exemplary is
式1的替代二氢嘧啶酮是中性粒细胞弹性蛋白酶抑制剂,可用作治疗COPD等疾病的药物。
Synthesis of 2-Substituted Furans by Iron- and Palladium-Catalyzed Coupling Reactions
synthesis of 2-substitutedfurans via palladium- and iron-catalyzed coupling utilizing 2-bromofuran is described. Whereas palladium-catalyzed Suzuki coupling effectively provided the corresponding aryl furans, little or no product was obtained by palladium-catalyzed coupling with various alkyl nucleophiles. Iron-catalyzed coupling proved effective for the synthesis of primary and secondary alkyl furans in modest
Analogs of dehydrophenylahistins and their therapeutic use
申请人:Palladino Michael
公开号:US20070078138A1
公开(公告)日:2007-04-05
Compounds represented by the following structure (II) are disclosed:
as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.
The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein.
The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.
This invention relates to compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling. The invention also provides compounds, compositions and methods for treating cell proliferative diseases and conditions and opthalmological diseases, disorders and conditions.