CO<sub>2</sub> as a C1 Source: B(C<sub>6</sub>F<sub>5</sub>)<sub>3</sub>-Catalyzed Cyclization of <i>o</i>-Phenylene-diamines To Construct Benzimidazoles in the Presence of Hydrosilane
作者:Zhenbei Zhang、Qiangsheng Sun、Chungu Xia、Wei Sun
DOI:10.1021/acs.orglett.6b03030
日期:2016.12.16
B(C6F5)3-catalyzed synthesis of benzimidazoles via cyclization of o-phenylenediamines with CO2 and PhSiH3. This metal-free catalytic route achieves the desired products in high yield under convenient reaction conditions and is applicable to a broad substrate scope. A plausible mechanism for the reaction involving a frustrated Lewis pair pathway is proposed based on spectroscopic characterization (e.g., 13C NMR) of
使用CO 2作为碳源催化构建苯并咪唑代表了获得这些有价值的化合物的简便且可持续的方法。在这里,我们描述了B(C 6 F 5)3催化的邻苯二胺与CO 2和PhSiH 3的环化反应,合成苯并咪唑。这种无金属的催化途径可以在方便的反应条件下以高收率获得所需的产物,并适用于广泛的底物范围。基于反应中间体的光谱表征(例如13 C NMR),提出了涉及沮丧的路易斯对途径的反应的合理机制。
[EN] NEW COMPOUNDS, PHARMACEUTICAL COMPOSITION AND METHODS RELATING THERETO<br/>[FR] NOUVEAUX COMPOSÉS, COMPOSITION PHARMACEUTIQUE ET PROCÉDÉS CORRESPONDANTS
申请人:BOEHRINGER INGELHEIM INT
公开号:WO2010149684A1
公开(公告)日:2010-12-29
New compounds are disclosed which have utility in the treatment of a variety of metabolic related conditions in a patient. The compounds of this invention have the structure (I): wherein R1, R2, R3, n, p, q, and Ar are as defined herein, including stereoisomers, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions comprising a compound of this invention, as well as methods relating to the use thereof in a patient in need thereof.
[EN] NOVEL PDE INHIBITORS, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND PROCESSES FOR THEIR PREPARATION<br/>[FR] NOUVEAUX INHIBITEURS DE PHOSPHODIESTÉRASES, COMPOSITIONS PHARMACEUTIQUES LES CONTENANT ET LEURS PROCÉDÉS DE PRÉPARATION
申请人:MATRIX LAB LTD
公开号:WO2009147476A1
公开(公告)日:2009-12-10
The present invention relates to novel heterocyclic compounds of general formula (I), which are phosphodiesterase inhibitors (PDEs), in particular phosphodiesterase type 4 inhibitors, pharmaceutical compositions containing them, and processes for their preparation. These novel PDEs are useful in treating allergic and inflammatory diseases (such as asthma, COPD, allergic rhinitis, allergic conjunctivitis, respiratory distress syndrome, chronic bronchitis, nephritis, rheumatoid spondylitis, osteoarthritis, atopic dermatitis, eosinophilic granuloma, psoriasis, rheumatoid septic shock, ulcerative colitis, multiple sclerosis, chronic inflammation, Crohn's syndrome and central nervous system(CNS) disorders) and for inhibiting the production of Tumor Necrosis Factor(TNF-α).
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Selected compounds are effective for prophylaxis and treatment of diseases, such as HGF mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable salts thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.