935862-97-8Relevant academic research and scientific papers
SUBSTITUTED FUSED HETEROARYL COMPOUND SERVING AS A KINASE INHIBITOR, AND APPLICATIONS THEREOF
-
Paragraph 0165, (2019/11/21)
The disclosure relates to substituted fused heteroaromatic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1-A4, B1-B3, D1-D4 and R1-R3 are defined herein. Compounds having Formula I are kinalse inhibitors. Therefore, compounds of the disclosure may be used to treat clinical conditions caused by DDR functional defects, such as cancer.
N-Heterocyclic carbene (NHC) catalyzed chemoselective acylation of alcohols in the presence of amines with various acylating reagents
Samanta, Ramesh C.,De Sarkar, Suman,Froehlich, Roland,Grimme, Stefan,Studer, Armido
, p. 2177 - 2184 (2013/05/21)
This edge article reports the synthesis and full characterization including X-ray analysis of three different acylazolium ions. The reactivity of these acylazolium ions as acylating reagents of amines and alcohols is discussed. Whereas benzylamine slowly reacts with the acylazolium ions, benzyl alcohol acylation does not occur. However, upon activation of the alcohol with an N-heterocyclic carbene (NHC) as catalyst, efficient esterification is achieved. Importantly, benzylester formation is obtained in the presence of benzylamine upon selective alcohol activation by the NHC. High level DFT calculations reveal that alcohol activation occurs by strong H-bond formation between the NHC and the alcohol thereby increasing the nucleophilicity of the alcohol. For oxidatively generated acylazolium ions under NHC catalysis, the carbene has a dual role (cooperative catalysis): (a) the NHC is used for generation of the acylazolium ion and (b) the NHC is used for activation of the alcohol in the subsequent acylation step. NHC-catalyzed selective acylation of benzyl alcohol in the presence of benzylamine can also be achieved with trifluoroethyl and hexafluoroisopropylesters as acylation reagents. Moreover, an enol acetate also shows high O-selectivity as a chemoselective acetylation reagent. Kinetic and mechanistic studies are provided and some examples of the chemoselective acylation of amino alcohols are presented.
ACYLATION REACTION OF HYDROXYL GROUP
-
Page/Page column 11, (2010/07/03)
Disclosed is a selective ester production process of an alcoholic hydroxyl group, which proceeds under chemically mild conditions, while having adequate environmental suitability, operability and economical efficiency. Specifically disclosed is a process for producing an ester compound, which is characterized in that an alcohol and a carboxylic acid ester compound are reacted in the presence of a compound containing zinc element, thereby selectively acylating a hydroxyl group of the alcohol.
COMPOUND CONTAINING BASIC GROUP AND USE THEREOF
-
Page/Page column 86, (2008/12/06)
The present invention relates to a compound represented by formula (I): wherein all symbols are as defined here, a salt thereof, a solvate thereof, or a prodrug thereof. The compound of the present invention has an antagonistic activity against CXCR4 and is therefore useful as a preventive and/or therapeutic agent for CXCR4-mediated diseases, for example, inflammatory and immune diseases (for example, rheumatoid arthritis, arthritis, retinopathy, pulmonary fibrosis, rejection of transplanted organ, etc.), allergic diseases, infections (for example, human immunodeficiency virus infection, acquired immunodeficiency syndrome, etc.), psychoneurotic diseases, cerebral diseases, cardiovascular disease, metabolic diseases, and cancerous diseases (for example, cancer, cancer metastasis, etc.), or an agent for regeneration therapy.
