Direct Cα-heteroarylation of structurally diverse ethers via a mild N-hydroxysuccinimide mediated cross-dehydrogenative coupling reaction
作者:Shihui Liu、Aoxia Liu、Yongqiang Zhang、Wei Wang
DOI:10.1039/c6sc05697k
日期:——
An important challenge in the Cα-heteroarylation of ethers is the requirement of a large excess amount of ethers (that are used as solvents in many cases) to achieve effective transformations. This drawback has significantly restricted the Cα-heteroarylation of ethers to the use of simple and easily accessible ether substrates. To overcome this limitation, a new, efficient, N-hydroxysuccinimide (NHS)
The invention provides quinazoline-7-ether derivatives, particularly 4-anilinyl-6-butenamido-quinazoline-7-ether derivatives that are inhibitors of the receptor protein tyrosine kinases (RTK). The compounds are useful in the treatment of diseases and disorders where RTK activity is implicated such as a hyperproliferative diseases (e.g., cancer). Also provided are methods of preparation of the quinazoline derivatives and methods of use as therapeutic agents alone or in a drug combination.
[EN] SUBSTITUTED HETEROARYL COMPOUNDS AND METHODS OF USE<br/>[FR] COMPOSÉS HÉTÉROARYLE SUBSTITUÉS ET LEURS MÉTHODES D'UTILISATION
申请人:SUNSHINE LAKE PHARMA CO LTD
公开号:WO2017048675A1
公开(公告)日:2017-03-23
The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.