60576-63-8Relevant academic research and scientific papers
Preparation method of 1, 3, 4-thiadiazole compound and compound prepared by preparation method
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Paragraph 0019-0020; 0063-0064, (2020/12/10)
The invention belongs to the field of medicinal chemistry. Specifically, the invention discloses a preparation method of a 1, 3, 4-thiadiazole compound and the compound prepared by using the preparation method. According to the method, the 1, 3, 4-thiadia
A KHSO4 promoted tandem synthesis of 1,3,4-thiadiazoles from thiohydrazides and DMF derivatives
Gan, Zongjie,Tian, Binghua,Yuan, Jianyong,Ran, Dongzhi,Zhang, Lin,Dong, Gang,Pan, Tao,Zeng, Yixin,Yu, Yu
supporting information, (2020/07/15)
An efficient, simple and environmentally benign method for the construction of 1,3,4-thiadiazole skeletons via the tandem coupling and cyclization of thiohydrazides with DMF derivatives in the presence of KHSO4 has been reported. This method re
Synthetic fermentation of β-peptide macrocycles by thiadiazole-forming ring-closing reactions
Hubert, Jonathan G.,Stepek, Iain A.,Noda, Hidetoshi,Bode, Jeffrey W.
, p. 2159 - 2167 (2018/03/05)
Macrocyclic β-peptides were efficiently prepared using a thiadiazole-forming cyclization reaction between an α-ketoacid and a thiohydrazide. The linear β-peptide precursors were assembled from isoxazolidine monomers by α-ketoacid-hydroxylamine (KAHA) ligations with a bifunctional initiator-a process we have termed 'synthetic fermentation' due to the analogy of producing natural product-like molecules from simpler building blocks. The linear synthetic fermentation products underwent Boc-deprotection/thiadiazole-forming macrocyclization under aqueous, acidic conditions to provide the cyclic products in a one-pot process. This reaction sequence proceeds from easily accessed initiator and monomer building blocks without the need for additional catalysts or reagents, enabling facile production of macrocyclic β-peptides, a relatively underexplored structural class.
