Wei Jianpeng, Li Yiming, Jiang Xuefeng
Shanghai Key Laboratory of Green Chemistry and Chemical Process, Department of Chemistry, East China Normal University , Shanghai 200062, P. R. China.
Beijing National Laboratory for Molecular Sciences (BNLMS) , Beijing 100190, P. R. China.
Org Lett. 2016 Jan 15;18(2):340-3. doi: 10.1021/acs.orglett.5b03541. Epub 2016 Jan 6.
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.
通过醛、硫化钠和N-取代甲酰胺实现了硫代酰胺的高效水相合成。烷基醛和芳基醛均适用于此方案。N-取代甲酰胺对于这种转化至关重要。易于获得的无机盐（硫化钠）在水中用作硫源，这使得该方法更加实用和高效。此外，已经建立了通过该方案对生物活性分子及其衍生物进行后期修饰的方法。
