The naturally and synthetically obtained 1,6-naphthyridine derivatives possess a wide range of pharmacological properties. This factor inspired the medicinal chemists and organic chemists to develop new methods for the synthesis of 1,6-naphthyridine derivatives. This review will discuss the synthesis of 1,6-naphthyridine and its derivatives from diverse starting materials or key intermediates in a systematic manner with appropriate mechanisms.
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