Aqueous Compatible Protocol to Both Alkyl and Aryl Thioamide Synthesis

An efficient aqueous synthesis of
thioamides through aldehydes,
sodium sulfide, and N-substituted formamides has
been developed. Both alkyl and aryl aldehydes are amenable to this
protocol. N-Substituted formamides are essential
for this transformation. Readily available inorganic salt (sodium
sulfide) serves as the sulfur source in water, which makes this method
much more practical and efficient. Furthermore, the late-stage modification
of bioactive molecules and derivatives through this protocol has been
established.