Facile Synthesis of Aryl - Pyridyl , P yridazinyl , Pyrazinyl , and Triazinyl Acetonitriles 585

Compounds containing aryl/heteroaryl acetic acid and aryl/heteroaryl ethylamine cores play important roles in the pharmaceutical field. Compounds containing aryl/heteroaryl acetic acid units form a large group of non-steroidal anti-inflammatory drugs such as Indomethacin [1], Diclophenac [2], Sulindac [3], Ketorolac [4], and many others. Also, this subunit appears in a number of antifungal [5], antiulcer [6], and anticancer compounds [7]. Aryl/heteroaryl ethylamine containing compounds show a variety of useful biological responses including antidiabetic [8], antiviral [9], antipsychotic [10], and anticonvulsant activities [11]. Recently, we required a convenient synthesis of substituted heteroaryl acetonitriles, which are important intermediates for the synthesis of several compounds within our drug discovery program. We report here a facile synthesis of substituted heteroaryl acetonitriles, which can be readily hydrolyzed to the corresponding acetic acids or reduced to form ethyl amine analogues that can serve as versatile precursors for the preparation of more complex molecules.