A highly efficient, elegant and chemoselective four-component one-pot protocol for the diversity-oriented synthesis of two type bioactive fused quinazolines via cyclocondensation has been studied. Diversity-oriented synthesis (DOS), efficient and simultaneous generation of chemical space with high degree of skeletal diversity, emerged a popular method in organic synthesis for generating diverse compound collection from readily accessible and common intermediates.1 The reaction demonstrates good tolerance of functional group and high yields. In particular, quinazolines are found in many synthetic drugs such as erlotinib, iressa and trazosin etc.2 On the other hand, pyrazole is a prevalent structure in many bio-active scaffolds such as fibronil, celecoxib, lonazolac and viagra etc.3 The salient features of the methods are broad substrate scope, good functional group tolerance and excellent regioslectivity. The results demonstrated that DOS methods contribute effectively in generating compound collection of small molecules for drug discovery and development.4

Synthesis of bioactive quinazolines by auto-tandem Pd(II) catalysis: A platform for Diversity Oriented Synthesis

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27th CRSI National Symposium in Chemistry

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