In this work, a highly efficient one-pot synthesis of 2,3,6trisubstituted pyridines has been achieved through coppercatalyzed saturated ketones and alkynones/1,3-dicarbonyl compounds. This method provided the convenient routes to the synthesis of 2,3,6-trisubstituted pyridines with good functional group tolerance. Compared with previous works, this method does not require the synthesis of enamine in advance.

A base‐mediated strategy was adopted to synthesize 2,4,6‐trisubstituted pyrimidines from amidine hydrochlorides, aldehydes and acetylacetone. The starting materials were widely available and could tolerate various functional groups, and the produced 2,4,6‐trisubstituted pyrimidines had moderate to good yields. The construction of C−C and C−N bonds was achieved under transition metal‐free conditions. Unlike previous approaches, the present approach utilizes a multicomponent reaction and is a new protocol for the construction of 2,4,6‐trisubstituted pyrimidines from raw materials that do not require further preparation.