1361234-46-9Relevant academic research and scientific papers
Facile approaches toward the synthesis of N4-monosubstituted quinazolin-2,4-diamines
Mohamed, Tarek,Rao, Praveen P.N.
, p. 6882 - 6885 (2015)
The amination of quinazoline-based heterocyclics is of significant interest due to its privileged structure and application in the development of bioactive compound libraries, as well as in the synthesis of readily convertible building blocks. The current approaches generally result in low yields, utilize harsh conditions, and/or rely on expensive catalysts. After examining three different approaches to synthesize N4-monosubstituted quinazolin-2,4-diamines, we developed an efficient and mild synthetic method to prepare quinazolin-2,4-diamines in 80-85% yields.
Synthesis of 2,4-diaminoquinazolines and tricyclic quinazolines by cascade reductive cyclization of methyl N -cyano-2-nitrobenzimidates
Yin, Ping,Liu, Nan,Deng, Yu-Xing,Chen, Yue,Deng, Yong,He, Ling
, p. 2649 - 2658 (2012/06/01)
An efficient route to N4-substituted 2,4-diaminoquinazolines has been developed by employing tandem condensation of cyanoimidate-amine and reductive cyclization in iron-HCl system. This method is tolerant of a following intramolecular N-alkylation and produces two fused heterocycles in a one-pot procedure. This protocol is a facile two-step synthesis of tricyclic quinazolines, which is effected by potent cyanoimidation and tandem reductive cyclization from 2-nitrobenzaldehydes. Moreover, the forming process of tricyclic quinazolines has been investigated from the ring-opening/ring-closing cascade point of view. It is found that the preparation of tricyclic quinazolinones in good yields relies on the selective hydrolysis of tricyclic quinazolines in base or acid system.
