Aqueous Compatible Protocol to Both Alkyl and Aryl Thioamide Synthesis

作者：Wei, Jianpeng; Li, Yiming; Jiang, Xuefeng^*

来源：Organic Letters, 2016, 18(2): 340-343.

DOI：10.1021/acs.orglett.5b03541

• LIGHT-INDUCED AMIDATION
• H BOND ACTIVATION
• METAL-FREE
• EFFICIENT
• ACID
• SULFUR
• DESULFURIZATION
• CONSTRUCTION
• THIONATION
• RADICALS

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.

• 出版日期2016-1-15
• 单位华东师范大学